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Discovery of a First-in-Class Small-Molecule Ligand for WDR91 Using DNA-Encoded Chemical Library Selection Followed by Machine Learning.
J Med Chem 66: 16051-16061 (2023)
University of Toronto
Serendipitous discovery of Class I HDAC inhibitors from rational design of molecular glue degraders targeting HDAC.
NA
Guizhou Medical University
Discovery of Anti-SARS-CoV-2 Nsp9 Binders from Natural Products by a Native Mass Spectrometry Approach.
J Nat Prod 86: 2630-2637 (2023)
Griffith University
Discovery of C-3 isoxazole substituted thiochromone S,S-dioxide derivatives as potent and selective inhibitors for monoamine oxidase B (MAO-B).
NA
University of South China
Discovery of (R)-4-(8-methoxy-2-methyl-1-(1-phenylethy)-1H-imidazo[4,5-c]quinnolin-7-yl)-3,5-dimethylisoxazole as a potent and selective BET inhibitor for treatment of acute myeloid leukemia (AML) guided by FEP calculation.
NA
Sichuan University
Identification of LY3522348: A Highly Selective and Orally Efficacious Ketohexokinase Inhibitor.
J Med Chem 66: 15960-15976 (2023)
Eli Lilly
Design, Synthesis, and Biological Evaluation of Trisubstituted Piperazine Derivatives as Noncovalent Severe Acute Respiratory Syndrome Coronavirus 2 Main Protease Inhibitors with Improved Antiviral Activity and Favorable Druggability.
J Med Chem 66: 16426-16440 (2023)
Shandong University
Design and Synthesis of Novel Cereblon Binders for Use in Targeted Protein Degradation.
J Med Chem 66: 16388-16409 (2023)
Bristol Myers Squibb
1,4-Benzothiazepines with Cyclopropanol Groups and Their Structural Analogues Exhibit Both RyR2-Stabilizing and SERCA2a-Stimulating Activities.
J Med Chem 66: 15761-15775 (2023)
Max Planck Institute for Multidisciplinary Sciences
Design, Synthesis, and Pharmacological Evaluation of Isoindoline Analogues as New HPK1 Inhibitors.
J Med Chem 66: 16201-16221 (2023)
Shanghai Jiao Tong University
Optimization of Novel α7 Nicotinic Acetylcholine Receptor Positive Allosteric Modulators and the Discovery of a Preclinical Development Candidate Molecule (RGH-560).
J Med Chem 66: 16276-16302 (2023)
Gedeon Richter
Dual inhibitors of HDAC and other epigenetic regulators: A novel strategy for cancer treatment.
NA
Guru Ghasidas University
HDAC specificity and kinase off-targeting by purine-benzohydroxamate anti-hematological tumor agents.
NA
University of Sao Paulo
Imidazolone as an Amide Bioisostere in the Development of β-1,3-
J Med Chem 66: 16120-16140 (2023)
Amgen
Discovery of triazole tethered thymol/carvacrol-coumarin hybrids as new class of α-glucosidase inhibitors with potent in vivo antihyperglycemic activities.
NA
Guru Nanak Dev University
Facilitating the development of molecular glues: Opportunities from serendipity and rational design.
NA
Sichuan University
Design, synthesis, and biological evaluation of 4-(2-fluorophenoxy)-7-methoxyquinazoline derivatives as dual EGFR/c-Met inhibitors for the treatment of NSCLC.
NA
Jiangxi Science & Technology Normal University
Review and prospects of targeted therapies for Spleen tyrosine kinase (SYK).
Bioorg Med Chem 96: (2023)
China Pharmaceutical University
Discovery of 5-(Pyrimidin-2-ylamino)-1
J Med Chem 66: 15847-15866 (2023)
Xiamen University
Discovery of Pyrazolo[1,5-
J Med Chem 66: 15944-15959 (2023)
China Pharmaceutical University
Discovery and Evaluation of C6-Substituted Pyrazolopyrimidine-Based Bisphosphonate Inhibitors of the Human Geranylgeranyl Pyrophosphate Synthase and Evaluation of Their Antitumor Efficacy in Multiple Myeloma, Pancreatic Ductal Adenocarcinoma, and Colorectal Cancer.
J Med Chem 66: 15776-15800 (2023)
Mcgill University
Discovery of Biaryl Amide Derivatives as Potent, Selective, and Orally Bioavailable RORγt Agonists for Cancer Immunotherapy.
J Med Chem 66: 16091-16108 (2023)
Fudan University
Highly potent dual-targeting angiotensin-converting enzyme 2 (ACE2) and Neuropilin-1 (NRP1) peptides: A promising broad-spectrum therapeutic strategy against SARS-CoV-2 infection.
NA
China Pharmaceutical University
Targeting SARS-CoV-2 entry processes: The promising potential and future of host-targeted small-molecule inhibitors.
NA
National Clinical Research Center for Geriatrics
5-(Trifluoromethyl)-1,2,4-oxadiazole (TFMO)-based highly selective class IIa HDAC inhibitors exhibit synergistic anticancer activity in combination with bortezomib.
NA
Heinrich Heine University Dusseldorf
4-Arylidene curcumin derivatives in vitro inhibit α-Synuclein aggregation and disaggregate the preformed fibril.
Bioorg Med Chem 96: (2023)
Zhengzhou University
Design, synthesis, and biological evaluation of deuterated indolepropionic acid derivatives as novel long-acting pan PPARα/γ/δ agonists.
Bioorg Med Chem 96: (2023)
Guangdong Pharmaceutical University
Discovery of a novel GPR35 agonist with high and equipotent species potency for oral treatment of IBD.
Bioorg Med Chem 96: (2023)
University of Chinese Academy of Sciences
In situ click chemistry-based discovery of 1,2,3-triazole-derived diarylpyrimidines as novel HIV-1 NNRTIs by exploiting the tolerant region I in binding pocket.
Bioorg Med Chem 96: (2023)
Shandong University
Discovery of potent chromone-based autotaxin inhibitors inspired by cannabinoids.
NA
European Molecular Biology Laboratory
Identification of selective 5-LOX and FLAP inhibitors as novel anti-inflammatory agents by ligand-based virtual screening.
NA
University of Naples "Federico II"
Development of a specific and potent IGF2BP1 inhibitor: A promising therapeutic agent for IGF2BP1-expressing cancers.
NA
Pennsylvania State University
Synthetic product-based approach toward potential antileishmanial drug development.
NA
Sangam University
Design, synthesis, ADME and biological evaluation of benzylpiperidine and benzylpiperazine derivatives as novel reversible monoacylglycerol lipase (MAGL) inhibitors.
NA
University of Pisa
Insight into the design of FGFR4 selective inhibitors in cancer therapy: Prospects and challenges.
NA
Jingzhou Hospital Affiliated to Yangtze University
Selective isoxazolopyrimidine PAT1 (SLC26A6) inhibitors for therapy of intestinal disorders.
RSC Med Chem 14: 2342-2347 (2023)
University of California
Designing photoaffinity tool compounds for the investigation of the DENV NS2B-NS3 protease allosteric binding pocket.
RSC Med Chem 14: 2365-2379 (2023)
Johannes Gutenberg-University
Past, present and future of xanthine oxidase inhibitors: design strategies, structural and pharmacological insights, patents and clinical trials.
RSC Med Chem 14: 2155-2191 (2023)
Guru Nanak Dev University
Discovery of carboxyl-containing heteroaryldihydropyrimidine derivatives as novel HBV capsid assembly modulators with significantly improved metabolic stability.
RSC Med Chem 14: 2380-2400 (2023)
Shandong University
Design, synthesis, and biological evaluation of diaminopyrimidine derivatives as novel focal adhesion kinase inhibitors.
RSC Med Chem 14: 2301-2314 (2023)
Shenyang Pharmaceutical University
The evolution of small molecule enzyme activators.
RSC Med Chem 14: 2206-2230 (2023)
University of Nebraska
Recent progress of small-molecule-based theranostic agents in Alzheimer's disease.
RSC Med Chem 14: 2231-2245 (2023)
Nanjing Tech University
Protease Inhibitors for Treating or Preventing Coronavirus Infection.
ACS Med Chem Lett 14: 1489-1490 (2023)
Smith, Gambrell & Russell
Development and Utilization of Novel Transglutaminase 2 Inhibitors for Potential Treatment of Autoimmune Disease and Gastrointestinal Disorder.
ACS Med Chem Lett 14: 1496-1497 (2023)
Usona Institute
Repurposing of Raltitrexed as an Effective G9a/EHMT2 Inhibitor and Promising Anti-Alzheimer's Agent.
ACS Med Chem Lett 14: 1531-1536 (2023)
National Institute of Technology Durgapur
Design of Novel Series of Antimalarial PMX Inhibitors with Increased Half-Life via Molecular Property Optimization.
ACS Med Chem Lett 14: 1582-1588 (2023)
Ucb
Novel 1,8-Naphthalimide Derivatives As Antitumor Agents and Potent Demethylase Inhibitors.
ACS Med Chem Lett 14: 1551-1557 (2023)
Nanjing Normal University
Small-Molecule Heterocyclic Compounds: Gq-Biased Agonists for the 5-HT2A Receptor in Neuropsychiatric Treatment.
ACS Med Chem Lett 14: 1498-1500 (2023)
Usona Institute
Novel Plasma Kallikrein Inhibitors for Treating Hereditary Angioedema, Diabetic Macular Edema, and Diabetic Retinopathy.
ACS Med Chem Lett 14: 1491-1492 (2023)
Smith, Gambrell & Russell
8-Aza Quinazolines as Brain Penetrant SOS1 Inhibitors for Treating Cancer.
ACS Med Chem Lett 14: 1487-1488 (2023)
Smith, Gambrell & Russell
Covalent Stapling of the Cereblon Sensor Loop Histidine Using Sulfur-Heterocycle Exchange.
ACS Med Chem Lett 14: 1576-1581 (2023)
Dana-Farber Cancer Institute
Emopamil-Binding Protein Inhibitors for Treating Multiple Sclerosis.
ACS Med Chem Lett 14: 1501-1502 (2023)
Smith, Gambrell & Russell
Identification of Ebselen derivatives as novel SARS-CoV-2 main protease inhibitors: Design, synthesis, biological evaluation, and structure-activity relationships exploration.
Bioorg Med Chem 96: (2023)
Shandong University
Development and Pharmacochemical Characterization Discover a Novel Brain-Permeable HDAC11-Selective Inhibitor with Therapeutic Potential by Regulating Neuroinflammation in Mice.
J Med Chem 66: 16075-16090 (2023)
Sichuan University
Optimization of mTOR Inhibitors Using Property-Based Drug Design and Free-Wilson Analysis for Improved In Vivo Efficacy.
ACS Med Chem Lett 14: 1544-1550 (2023)
Takeda California
Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers.
J Med Chem 66: 15629-15647 (2023)
Kronos Bio
Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N-Terminal Bromodomain Chemical Probe.
J Med Chem 66: 15728-15749 (2023)
Gsk
Discovery of PVD-06 as a Subtype-Selective and Efficient PTPN2 Degrader.
J Med Chem 66: 15269-15287 (2023)
Shanghai Institute of Materia Medica
Discovery of Orally Bioavailable Phthalazinone Analogues as an ENPP1 Inhibitor for STING-Mediated Cancer Immunotherapy.
J Med Chem 66: 15141-15170 (2023)
Ajou University
Conformationally constrained potent inhibitors for enhancer of zeste homolog 2 (EZH2).
NA
Shanghai Synergy Pharmaceutical Sciences Co., Ltd.
Discovery of novel indole derivatives as potent and selective inhibitors of proMMP-9 activation.
NA
Taisho Pharmaceutical Co., Ltd.
Design, synthesis and biological evaluation of EGFR kinase inhibitors that spans the orthosteric and allosteric sites.
Bioorg Med Chem 96: (2023)
Zunyi Medical University
Target discovery of bioactive natural products with native-compound-coupled CNBr-activated Sepharose 4B beads (NCCB): Applications, mechanisms and outlooks.
Bioorg Med Chem 96: (2023)
Zhengzhou University
New aryl-/heteroarylpiperazine derivatives of 1,7-dimethyl-8,9-diphenyl-4-azatricyclo[5.2.1.0
Bioorg Med Chem 96: (2023)
Medical University of Warsaw
Discovery of benzamide-based PI3K/HDAC dual inhibitors with marked pro-apoptosis activity in lymphoma cells.
NA
Ocean University of China
Synthesis and clinical application of small-molecule drugs approved to treat prostatic cancer.
NA
Zhengzhou Normal University
Identification and Optimization of Novel Inhibitors of the Polyketide Synthase 13 Thioesterase Domain with Antitubercular Activity.
J Med Chem 66: 15380-15408 (2023)
University of Dundee
Discovery of 3-oxo-1,2,3,4-tetrahydropyrido[1,2-a]pyrazin derivatives as SARS-CoV-2 main protease inhibitors through virtual screening and biological evaluation.
NA
Peking University
Discovery of PFI-6, a small-molecule chemical probe for the YEATS domain of MLLT1 and MLLT3.
Bioorg Med Chem Lett 98: (2024)
University of Oxford
Discovery of novel dual Bruton's tyrosine kinase (BTK) and Janus kinase 3 (JAK3) inhibitors as a promising strategy for rheumatoid arthritis.
Bioorg Med Chem 96: (2023)
China Pharmaceutical University
Unlocking the synthetic approaches and clinical application of approved small-molecule drugs for gastrointestinal cancer treatment: A comprehensive exploration.
NA
KU Leuven
Open science discovery of potent noncovalent SARS-CoV-2 main protease inhibitors.
Science 382: (2023)
Cornell University
Design, Synthesis, and Biological Evaluation of an Orally Bioavailable, Potent, and Selective ROCK2 Inhibitor for Psoriasis Treatment.
J Med Chem 66: 15205-15229 (2023)
Zhejiang University
Development of N-Terminally Modified Variants of the CXCR4-Antagonistic Peptide EPI-X4 for Enhanced Plasma Stability.
J Med Chem 66: 15189-15204 (2023)
Ulm University Medical Center
Design and synthesis of sirtinol analogs as human neutrophil elastase inhibitors.
NA
Chang Gung University
Discovery of a novel tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid derivative as a potent and selective heparanase-1 inhibitor utilizing an improved synthetic approach.
NA
Taisho Pharmaceutical Co, Ltd
Identification of benzothiazoles as novel PCSK9 inhibitors.
NA
Hebei Normal University
Harvesting phosphorus-containing moieties for their antibacterial effects.
Bioorg Med Chem 96: (2023)
University of Helsinki
Synthesis, biological evaluation and action mechanism of 7H-[1,2,4] triazolo [3,4-b] [1,3,4] thiadiazine-phenylhydrazone derivatives as α-glucosidase inhibitors.
NA
The Affiliated Hospital of Guizhou Medical University
Discovery of a Hydroxylamine-Based Brain-Penetrant EGFR Inhibitor for Metastatic Non-Small-Cell Lung Cancer.
J Med Chem 66: 15477-15492 (2023)
University of Georgia
Discovery of a potent and selective human AC2 inhibitor based on 7-deazapurine analogues of adefovir.
Bioorg Med Chem 95: (2023)
University of Chemistry and Technology Prague
Advances in nitric oxide regulators for the treatment of ischemic stroke.
NA
China Pharmaceutical University
Discovery of novel tumor-targeted near-infrared probes with 6-substituted pyrrolo[2,3-d]pyrimidines as targeting ligands.
NA
Hebei Medical University
Synthesis, anti-inflammatory activity, and conformational relationship studies of chromone derivatives incorporating amide groups.
Bioorg Med Chem Lett 96: (2023)
Inner Mongolia Medical University
Synthetic approaches and application of clinically approved small-molecule drugs to treat hepatitis.
NA
Children's Hospital Affiliated to Zhengzhou University
Design and synthesis of certain 7-Aryl-2-Methyl-3-Substituted Pyrazolo{1,5-a}Pyrimidines as multikinase inhibitors.
NA
Sana'a University
A potent and selective cis-amide inhibitor of ryanodine receptor 2 as a candidate for cardiac arrhythmia treatment.
NA
Tokyo Medical and Dental University (TMDU)
Covalent Peptide LSD1 Inhibitor Specifically Recognizes Cys360 in the Enzyme-Active Region.
J Med Chem 66: 15409-15423 (2023)
Shenzhen University
Design, Synthesis, and Pharmacological Evaluation of Multisubstituted Pyrido[4,3-
J Med Chem 66: 15524-15549 (2023)
Shanghai Jiao Tong University
Exploring Fatty Acid Mimetics as NR4A Ligands.
J Med Chem 66: 15362-15369 (2023)
Ludwig Maximilian University of Munich
Drug repurposing and structure-based discovery of new PDE4 and PDE5 inhibitors.
NA
Chinese Academy of Sciences
Insight from Linker Investigations: Discovery of a Novel Phenylbenzothiazole Necroptosis Inhibitor Targeting Receptor-Interacting Protein Kinase 1 (RIPK1) from a Phenoxybenzothiazole Compound with Dual RIPK1/3 Targeting Activity.
J Med Chem 66: 15288-15308 (2023)
Zhejiang University
Direct evaluation of polarity of the ligand binding pocket in retinoid X receptor using a fluorescent solvatochromic agonist.
Bioorg Med Chem Lett 96: (2023)
Okayama University
Further Studies on the Highly Active Des-C-Ring and Aromatic-D-Ring Analogues of 1α,25-Dihydroxyvitamin D
J Med Chem 66: 15326-15339 (2023)
University of Santiago De Compostela
Resveratrol Derivatives Inhibit Transthyretin Fibrillization: Structural Insights into the Interactions between Resveratrol Derivatives and Transthyretin.
J Med Chem 66: 15511-15523 (2023)
University of Toyama
Agents for the Treatment of Gout: Current Advances and Future Perspectives.
J Med Chem 66: 14474-14493 (2023)
Shenyang Pharmaceutical University
Design of a Supersoft Topical JAK Inhibitor, Which Is Effective in Human Skin but Rapidly Deactivated in Blood.
J Med Chem 66: 15042-15053 (2023)
Novartis Institutes For Biomedical Research
Structure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors.
J Med Chem 66: 14866-14896 (2023)
Leibniz-Fmp
Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation.
J Med Chem 66: 14787-14814 (2023)
Leipzig University
4-(3-Phenyl-4-(3,4,5-trimethoxybenzoyl)-1
J Med Chem 66: 14824-14842 (2023)
Catholic University of The Sacred Heart
Leveraging Ligand Affinity and Properties: Discovery of Novel Benzamide-Type Cereblon Binders for the Design of PROTACs.
J Med Chem 66: 14513-14543 (2023)
University of Bonn
Design, synthesis and preclinical evaluation of muscarine receptor antagonists via a scaffold-hopping approach.
NA
University of Vienna
Structure-Activity Relationship and Biological Investigation of a REV-ERBα-Selective Agonist SR-29065 (
J Med Chem 66: 14815-14823 (2023)
The Scripps Research Institute
Discovery of Novel Fourth-Generation EGFR Inhibitors to Overcome C797S-Mediated Resistance.
J Med Chem 66: 14633-14652 (2023)
China Pharmaceutical University
Covalent and noncovalent strategies for targeting Lys102 in HIV-1 reverse transcriptase.
NA
Yale University
Small-molecule inhibitors targeting apoptosis signal-regulated kinase 1.
NA
Jiangxi University of Chinese Medicine
Discovery of 3-Phenyl Indazole-Based Novel Chemokine-like Receptor 1 Antagonists for the Treatment of Psoriasis.
J Med Chem 66: 14564-14582 (2023)
Gwangju Institute of Science and Technology (GIST)
Recent Progress and Prospects of Small Molecules for NLRP3 Inflammasome Inhibition.
J Med Chem 66: 14447-14473 (2023)
Sichuan University
Ligand Sulfur Oxidation State Progressively Alters Galectin-3-Ligand Complex Conformations To Induce Affinity-Influencing Hydrogen Bonds.
J Med Chem 66: 14716-14723 (2023)
Lund University
Hydroxamic acid hybrids: Histone deacetylase inhibitors with anticancer therapeutic potency.
NA
Shandong University
Integrating Taxonomic and Chemical Diversity of Mangrove-Associated Ascomycetes to Discover or Repurpose Bioactive Natural Products.
J Nat Prod 86: 2423-2434 (2023)
National Autonomous University of Mexico
Fused Tetrahydroquinolines Are Interfering with Your Assay.
J Med Chem 66: 14434-14446 (2023)
University of North Carolina at Chapel Hill
Discovery of Clinical Candidate NT-0796, a Brain-Penetrant and Highly Potent NLRP3 Inflammasome Inhibitor for Neuroinflammatory Disorders.
J Med Chem 66: 14897-14911 (2023)
Nodthera
Sticklac-Derived Natural Compounds Inhibiting RNase H Activity of HIV-1 Reverse Transcriptase.
J Nat Prod 86: 2487-2495 (2023)
Chiba University
Expanding the squaramide library as mycobacterial ATP synthase inhibitors: Innovative synthetic pathway and biological evaluation.
Bioorg Med Chem 95: (2023)
Palacky University
An updated review of chemical compounds with anti-Toxoplasma gondii activity.
NA
Universidad de Buenos Aires
Multi-targeted anti-Alzheimer's agents: Synthesis, biological evaluation, and molecular modeling study of some pyrazolopyridine hybrids.
NA
Mansoura University
Dual Inhibition of
J Med Chem 66: 14724-14734 (2023)
University of North Carolina at Chapel Hill
Discovery and Optimization of Novel
J Med Chem 66: 14755-14786 (2023)
Sichuan University
Discovery of Selective and Potent Macrocyclic CDK9 Inhibitors for the Treatment of Osimertinib-Resistant Non-Small-Cell Lung Cancer.
J Med Chem 66: 15340-15361 (2023)
China Pharmaceutical University
Imidazo[2,1-b]thiazole based indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor: Structure based design, synthesis, bio-evaluation and docking studies.
Bioorg Med Chem Lett 96: (2023)
Panjab University
Pyrazolidinone-based peptidomimetic SARS-CoV-2 M
Bioorg Med Chem Lett 96: (2023)
Latvian Institute of Organic Synthesis
Identification of novel glucocerebrosidase chaperones by unexpected skeletal rearrangement reaction.
Bioorg Med Chem Lett 96: (2023)
Eisai
The location, physiology, pathology of hippocampus Melatonin MT2 receptor and MT2-selective modulators.
NA
The First Affiliated Hospital of China Medical University
Synthetic non-toxic anti-biofilm agents as a strategy in combating bacterial resistance.
NA
Pharmaceutical and Drug Industries Research Institute
Discovery of benzimidazole-indazole derivatives as potent FLT3-tyrosine kinase domain mutant kinase inhibitors for acute myeloid leukemia.
NA
Gwangju Institute of Science and Technology (GIST)
Analysis of structure-activity relationship of indol-3-yl-N-phenylcarbamic amides as potent STING inhibitors.
Bioorg Med Chem 95: (2023)
National Health Research Institutes
Design, Synthesis, and Evaluation of
Bioorg Med Chem Lett 96: (2023)
Chongqing Medical University
Design, synthesis and anticancer activity evaluation of 4-(3-1H-indazolyl)amino quinazoline derivatives as PAK4 inhibitors.
Bioorg Med Chem 95: (2023)
China Pharmaceutical University
Discovery of novel amidobenzimidazole derivatives as orally available small molecule modulators of stimulator of interferon genes for cancer immunotherapy.
NA
Korea Research Institute of Chemical Technology
Design, synthesis and biological evaluation of novel DCLK1 inhibitor containing purine skeleton for the treatment of pancreatic cancer.
NA
China Pharmaceutical University
Dual COX-2/15-LOX inhibitors: A new avenue in the prevention of cancer.
NA
Islamic Azad University
First Optimization of Novel, Potent, Selective PDE11A4 Inhibitors for Age-Related Cognitive Decline.
J Med Chem 66: 14597-14608 (2023)
Montclair State University
Discovery of MK-1468: A Potent, Kinome-Selective, Brain-Penetrant Amidoisoquinoline LRRK2 Inhibitor for the Potential Treatment of Parkinson's Disease.
J Med Chem 66: 14912-14927 (2023)
Merck
Synthesis and Bioevaluation of 3-(Arylmethylene)indole Derivatives: Discovery of a Novel ALK Modulator with Antiglioblastoma Activities.
J Med Chem 66: 14609-14622 (2023)
Nanjing Medical University
Structure-Based Optimization and Biological Evaluation of Potent and Selective MMP-7 Inhibitors for Kidney Fibrosis.
J Med Chem 66: 14653-14668 (2023)
Taisho Pharmaceutical Co.
Screening and optimization of phage display cyclic peptides against the WDR5 WBM site.
RSC Med Chem 14: 2048-2057 (2023)
University of Chinese Academy of Sciences
MEK inhibitors in cancer treatment: structural insights, regulation, recent advances and future perspectives.
RSC Med Chem 14: 1837-1857 (2023)
Central University of Punjab
Exploration of tricyclic heterocycles as core structures for RIOK2 inhibitors.
RSC Med Chem 14: 2007-2011 (2023)
Jinan University
Synthesis, activity and metabolic stability of propan-2-one substituted tetrazolylalkanoic acids as dual inhibitors of cytosolic phospholipase A
RSC Med Chem 14: 2079-2088 (2023)
University of Muenster
Identification of novel 1,2,3-triazole isatin derivatives as potent SARS-CoV-2 3CLpro inhibitors
RSC Med Chem 14: 2068-2078 (2023)
Shandong University
The rational design of ARUK2007145, a dual inhibitor of the α and γ isoforms of the lipid kinase phosphatidylinositol 5-phosphate 4-kinase (PI5P4K).
RSC Med Chem 14: 2035-2047 (2023)
University of Cambridge
Targeting NOX2 with Bivalent Small-Molecule p47phox-p22phox Inhibitors.
J Med Chem 66: 14963-15005 (2023)
University of Copenhagen
Photoswitchable Probes of Oxytocin and Vasopressin.
J Med Chem 66: 14853-14865 (2023)
University of Regensburg
Receptor Interacting Ser/Thr-Protein Kinase 2 as a New Therapeutic Target.
J Med Chem 66: 14391-14410 (2023)
University of Lille
ATP ion channel P2X7 receptor as a regulatory molecule in the progression of colorectal cancer.
NA
Nanchang University
Interleukin-1β converting enzyme (ICE): A comprehensive review on discovery and development of caspase-1 inhibitors.
NA
L J University Ahmedabad
Catecholamine Derivatives: Natural Occurrence, Structural Diversity, and Biological Activity.
J Nat Prod 86: 2592-2619 (2023)
Shandong University
Design, Synthesis, and Antitumor Efficacy of Substituted 2-Amino[1,2,4]triazolopyrimidines and Related Heterocycles as Dual Inhibitors for Microtubule Polymerization and Janus Kinase 2.
J Med Chem 66: 15006-15024 (2023)
Wuyi University
Novel Pyrazolopyrazine Compounds as SHP2 Inhibitors for Treating Glioblastoma.
ACS Med Chem Lett 14: 1336-1337 (2023)
Smith, Gambrell & Russell
Design and Optimization of Novel Competitive, Non-peptidic, SARS-CoV-2 M
ACS Med Chem Lett 14: 1434-1440 (2023)
Emory University
Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors.
ACS Med Chem Lett 14: 1351-1357 (2023)
Erasca
Structure-Activity Relationships of Cyano-substituted Indole Derivatives as Ligands for α-Synuclein Aggregates.
ACS Med Chem Lett 14: 1467-1471 (2023)
Beijing Normal University
Expanding the Chemical Space: New Approach to Cell-Permeable Drugs.
ACS Med Chem Lett 14: 1329-1330 (2023)
Usona Institute
Fragment-Based NMR Screening of the BPTF PHD Finger Methyl Lysine Reader Leads to the First Small-Molecule Inhibitors.
ACS Med Chem Lett 14: 1441-1447 (2023)
University of Minnesota
Targeting the Inhibition of B-Cell Lymphoma 2 Protein for the Treatment of Cancer.
ACS Med Chem Lett 14: 1320-1322 (2023)
Therachem Research Medilab
Emopamil-Binding Protein Inhibitors for Treating Multiple Sclerosis.
ACS Med Chem Lett 14: 1318-1319 (2023)
Smith, Gambrell & Russell
Interplay of Modified Sialic Acid Inhibitors and the Human Parainfluenza Virus 1 Hemagglutinin-Neuraminidase Active Site.
ACS Med Chem Lett 14: 1383-1388 (2023)
University of Milan
Novel Indazole Compounds as TEAD Inhibitors for Treating Cancer.
ACS Med Chem Lett 14: 1334-1335 (2023)
Smith, Gambrell & Russell
Design of Next-Generation DGAT2 Inhibitor PF-07202954 with Longer Predicted Half-Life.
ACS Med Chem Lett 14: 1427-1433 (2023)
Pfizer
Discovery of Pyrrolo[2,3-
ACS Med Chem Lett 14: 1389-1395 (2023)
University of Michigan
Unleashing the Potential of 1,3-Diketone Analogues as Selective LH2 Inhibitors.
ACS Med Chem Lett 14: 1396-1403 (2023)
University of Texas At Austin
Synthesis and Optimization of 1-Substituted Imidazo[4,5-
ACS Med Chem Lett 14: 1358-1368 (2023)
Binghamton University School of Pharmacy and Pharmaceutical Sciences
The mechanisms of multidrug resistance of breast cancer and research progress on related reversal agents.
Bioorg Med Chem 95: (2023)
University of South China
Discovery of Selective Histone Deacetylase 1 and 2 Inhibitors: Screening of a Focused Library Constructed by Click Chemistry, Kinetic Binding Analysis, and Biological Evaluation.
J Med Chem 66: 15171-15188 (2023)
Osaka University
Diamino Allose Phosphates: Novel, Potent, and Highly Stable Toll-like Receptor 4 Agonists.
J Med Chem 66: 13900-13917 (2023)
Inimmune
Discovery of Quinazoline-2,4(1
J Med Chem 66: 14095-14115 (2023)
Chinese Academy of Medical Sciences and Peking Union Medical College
Discovery and Synthesis of a Naturally Derived Protein Kinase Inhibitor that Selectively Inhibits Distinct Classes of Serine/Threonine Kinases.
J Nat Prod 86: 2283-2293 (2023)
National Cancer Institute
Discovery of a novel BLT2 antagonist for the treatment of inflammatory airway diseases.
NA
Korea University
Development of potent isoflavone-based formyl peptide receptor 1 (FPR1) antagonists and their effects in gastric cancer cell models.
Eur J Med Chem 261: (2023)
University of Bari Aldo Moro
Small molecules targeting molecular chaperones for tau regulation: Achievements and challenges.
NA
China Pharmaceutical University
Modification of osimertinib to discover new potent EGFRC797S-TK inhibitors.
NA
Xi'an Jiaotong University
Reading and erasing of histone crotonyllysine mimics by the AF9 YEATS domain and SIRT2 deacylase.
Bioorg Med Chem 95: (2023)
University of Southern Denmark
Design, Synthesis, and Biological Evaluation of Novel Thioureidobenzamide (TBA) Derivatives as HBV Capsid Assembly Modulators.
J Med Chem 66: 13968-13990 (2023)
Weifang Medical University
Discovery and characterisation of quinazolines and 8-Azaquinazolines as NLRP3 agonists with oral bioavailability in mice.
Bioorg Med Chem Lett 96: (2023)
Astrazeneca
Design, synthesis and biological evaluation of 2-aminopyrimidine derivatives as potent FLT3 inhibitors.
Bioorg Med Chem Lett 96: (2023)
Zhejiang University
Development of small molecule inhibitors targeting RNA helicase DHX33 as anti-cancer agents.
Bioorg Med Chem Lett 96: (2023)
Shenzhen Keye Life Technologies Co.
Discovery of novel multifunctional ligands targeting GABA transporters, butyrylcholinesterase, β-secretase, and amyloid β aggregation as potential treatment of Alzheimer's disease.
Eur J Med Chem 261: (2023)
Jagiellonian University Medical College
PITB: A high affinity transthyretin aggregation inhibitor with optimal pharmacokinetic properties.
Eur J Med Chem 261: (2023)
Autonomous University of Barcelona
Design, synthesis, and biological evaluation of novel 4,4'-bipyridine derivatives acting as CDK9-Cyclin T1 protein-protein interaction inhibitors against triple-negative breast cancer.
NA
Xiamen University
Imidazole-based sphingosine-1-phosphate transporter Spns2 inhibitors.
Bioorg Med Chem Lett 96: (2023)
Virginia Tech
Indirubin derivatives as bifunctional molecules inducing DNA damage and targeting PARP for the treatment of cancer.
NA
China Pharmaceutical University
Inhibiting HCMV pUL89-C Endonuclease with Metal-Binding Compounds.
J Med Chem 66: 13874-13887 (2023)
University of Minnesota
Non-peptidic immunoproteasome β5i-selective inhibitor as potential treatment for idiopathic pulmonary fibrosis: Virtual screening, hit evolution and lead identification.
NA
Chinese Academy of Medical Sciences & Peking Union Medical College
Discovery of dihydropyridinone derivative as a covalent EZH2 degrader.
NA
Chinese Academy of Sciences
Exploring the structural-activity relationship of hexahydropyrazino[1,2-d]pyrido[3,2-b][1,4]oxazine derivatives as potent and orally-bioavailable PARP7 inhibitors.
NA
Guizhou University
Targeting the Tyrosine Kinase 2 (TYK2) Pseudokinase Domain: Discovery of the Selective TYK2 Inhibitor ABBV-712.
J Med Chem 66: 14335-14356 (2023)
Abbvie
Structural Basis for Highly Selective Class II Alpha Phosphoinositide-3-Kinase Inhibition.
J Med Chem 66: 14278-14302 (2023)
Leibniz-Fmp
Chemical exploration of TGR5 functional hot-spots: Synthesis and structure-activity relationships of C7- and C23-Substituted cholic acid derivatives.
Eur J Med Chem 261: (2023)
Tes Pharma
Discovery and structural optimization of a new series of N-acyl-2-aminobenzothiazole as inhibitors of Zika virus.
Bioorg Med Chem 95: (2023)
Federal University of Uberlandia (UFU)
Design, synthesis, and biological evaluation of a novel series of 1,2,4-oxadiazole inhibitors of SLACK potassium channels: Identification of in vitro tool VU0935685.
Bioorg Med Chem 95: (2023)
University of North Texas Health Science Center
Strategies for the Discovery of Oxazolidinone Antibacterial Agents: Development and Future Perspectives.
J Med Chem 66: 13860-13873 (2023)
Sichuan University
Fluorinated aldosterone synthase (CYP11B2)-inhibitors for differential diagnosis between bilateral and unilateral conditions of primary aldosteronism.
Bioorg Med Chem Lett 96: (2023)
University Hospital of Wuerzburg
Development of chalcone-like derivatives and their biological and mechanistic investigations as novel influenza nuclear export inhibitors.
NA
Shandong University
Synthesis and application of small molecules approved for the treatment of lymphoma.
NA
The First Affiliated Hospital of Zhengzhou University
Discovery and optimization of indirubin derivatives as novel ferroptosis inducers for the treatment of colon cancer.
NA
China Pharmaceutical University
Design and synthesis of 1H-benzo[d]imidazole selective HDAC6 inhibitors with potential therapy for multiple myeloma.
NA
Sichuan University
Selective and Bioavailable HDAC6 2-(Difluoromethyl)-1,3,4-oxadiazole Substrate Inhibitors and Modeling of Their Bioactivation Mechanism.
J Med Chem 66: 14188-14207 (2023)
Astrazeneca
Superiority of the Triple-Acting 5-HT
J Med Chem 66: 14928-14947 (2023)
Jagiellonian University Medical College
Diterpenoids from
J Nat Prod 86: 2379-2390 (2023)
Huazhong University of Science and Technology
Discovery of Novel Fedratinib-Based HDAC/JAK/BRD4 Triple Inhibitors with Remarkable Antitumor Activity against Triple Negative Breast Cancer.
J Med Chem 66: 14150-14174 (2023)
Shandong University
-(2-Aminophenyl)-benzamide Inhibitors of Class I HDAC Enzymes with Antiproliferative and Antifibrotic Activity.
J Med Chem 66: 14357-14376 (2023)
National and Kapodistrian University of Athens
Structure-Based Design of a Lead Compound Derived from Natural Schweinfurthins with Antitumor Properties That Target Oxysterol-Binding Protein.
J Med Chem 66: 14208-14220 (2023)
University Paris-Saclay
Integrated fragment-based drug design and virtual screening techniques for exploring the antidiabetic potential of thiazolidine-2,4-diones: Design, synthesis and in vivo studies.
NA
ISF College of Pharmacy
Synthesis and clinical application of small-molecule inhibitors of Janus kinase.
NA
Zhengzhou Normal University
Discovery of novel G9a/GLP covalent inhibitors for the treatment of triple-negative breast cancer.
NA
Sichuan University
Design and synthesis of 4th generation EGFR inhibitors against human triple (Del19/T790M/C797S) mutation.
NA
Sungkyunkwan University
Design, synthesis and biological evaluation of novel 2,4-thiazolidinedione derivatives able to target the human BAG3 protein.
Eur J Med Chem 261: (2023)
Aptuit An Evotec
Difluoromethyl-1,3,4-oxadiazoles Are Selective, Mechanism-Based, and Essentially Irreversible Inhibitors of Histone Deacetylase
J Med Chem 66: 13821-13837 (2023)
University of Bonn
Discovery of a 53BP1 Small Molecule Antagonist Using a Focused DNA-Encoded Library Screen.
J Med Chem 66: 14133-14149 (2023)
University of North Carolina at Chapel Hill
Development of small molecule inhibitors of natural killer group 2D receptor (NKG2D).
Bioorg Med Chem Lett 96: (2023)
Janssen Research & Development
Inhibition of Son of Sevenless Homologue 1 (SOS1): Promising therapeutic treatment for KRAS-mutant cancers.
NA
China Pharmaceutical University
Evaluation of novel pyrazol-4-yl pyridine derivatives possessing arylsulfonamide tethers as c-Jun N-terminal kinase (JNK) inhibitors in leukemia cells.
NA
Modern University for Technology and Information (MTI)
Strategies for developing retinoic acid receptor alpha-selective antagonists as novel agents for male contraception.
NA
University of Minnesota
Structure-activity relationship studies and biological properties evaluation of peptidic NRP-1 ligands: Investigation of N-terminal cysteine importance.
Bioorg Med Chem 94: (2023)
University of Warsaw
Selective modifications of lactose and N-acetyllactosamine with sulfate and aromatic bulky groups unveil unique structural insights in galectin-1-ligand recognition.
Bioorg Med Chem 94: (2023)
Instituto De Biologia Y Medicina Experimental (IBYME)
Identification of GDC-1971 (RLY-1971), a SHP2 Inhibitor Designed for the Treatment of Solid Tumors.
J Med Chem 66: 13384-13399 (2023)
Relay Therapeutics
SARS-CoV-2 papain-like protease (PLpro) inhibitory and antiviral activity of small molecule derivatives for drug leads.
Bioorg Med Chem Lett 96: (2023)
Purdue University
Discovery of a Novel Ketohexokinase Inhibitor with Improved Drug Distribution in Target Tissue for the Treatment of Fructose Metabolic Disease.
J Med Chem 66: 13501-13515 (2023)
Tuojie Biotech (Shanghai) Co.
Discovery of Triazinone Derivatives as Novel, Specific, and Direct NLRP3 Inflammasome Inhibitors for the Treatment of DSS-Induced Ulcerative Colitis.
J Med Chem 66: 13428-13451 (2023)
Sichuan University
Structure-Activity Relationship Studies of SARS-CoV-2 Main Protease Inhibitors Containing 4-Fluorobenzothiazole-2-carbonyl Moieties.
J Med Chem 66: 13516-13529 (2023)
Tokyo Medical and Dental University (TMDU)
Identification of a Novel, Potent, and Orally Bioavailable Guanidine-Based SHP2 Allosteric Inhibitor from Virtual Screening and Rational Structural Optimization for the Treatment of KRAS Mutant Cancers.
J Med Chem 66: 13646-13664 (2023)
China Pharmaceutical University
Construction and Evaluation of Novel Dual-function Antifungal Inhibitors and Covalent Organic Framework Carriers Based on the Infection Microenvironment.
J Med Chem 66: 13838-13857 (2023)
Liaocheng University
Expanding the Role of Boron in New Drug Chemotypes: Properties, Chemistry, Pharmaceutical Potential of Hemiboronic Naphthoids.
J Med Chem 66: 13768-13787 (2023)
University of Alberta
Structure-Guided Design of Nurr1 Agonists Derived from the Natural Ligand Dihydroxyindole.
J Med Chem 66: 13556-13567 (2023)
Ludwig Maximilian University of Munich
Design, Synthesis, and Biological Evaluation of Proteolysis-Targeting Chimeras as Highly Selective and Efficient Degraders of Extracellular Signal-Regulated Kinase 5.
J Med Chem 66: 13568-13586 (2023)
Peking University
Discovery of Novel Oxazepine Derivatives as Akt/ROCK Inhibitors for Growth Arrest and Differentiation Induction in Neuroblastoma Treatment.
J Med Chem 66: 13530-13555 (2023)
Zhejiang University
Exploring novel anticancer pyrazole benzenesulfonamides featuring tail approach strategy as carbonic anhydrase inhibitors.
NA
Cairo University
Design of a structure-activity relationship model of vitamin K epoxide reductase (VKORC1) inhibitors combining chemical synthesis of new compounds, enzymatic assays and molecular modelling.
Bioorg Med Chem 94: (2023)
University of Lyon
Discovery of potential novel TRPC5 inhibitors by virtual screening and bioassay.
Bioorg Med Chem 94: (2023)
Chinese Academy of Sciences
Discovery of the Potent and Selective Inhaled Janus Kinase 1 Inhibitor AZD4604 and Its Preclinical Characterization.
J Med Chem 66: 13400-13415 (2023)
Astrazeneca
Unlocking DCAFs To Catalyze Degrader Development: An Arena for Innovative Approaches.
J Med Chem 66: 13369-13383 (2023)
Baylor College of Medicine
Chemical Analysis and Antidiabetic Potential of a Decoction from
J Nat Prod 87: 501-513 (2024)
National Autonomous University of Mexico
Novel P2X3 Inhibitors for Treating Neurogenic Disorders.
ACS Med Chem Lett 14: 1146-1147 (2023)
Smith, Gambrell & Russell
Synthesis and Validation of the First Cell-Impermeable Hsp90α-Selective Inhibitors.
ACS Med Chem Lett 14: 1250-1256 (2023)
The University of Notre Dame
Molecular Design of Cyclic Peptides with Cell Membrane Permeability and Development of MDMX-p53 Inhibitor.
ACS Med Chem Lett 14: 1174-1178 (2023)
Fujifilm
Dose-Response Activity-Based DNA-Encoded Library Screening.
ACS Med Chem Lett 14: 1295-1303 (2023)
The Scripps Research Institute
Novel Compounds for Preventing SARS-CoV-2 Viral Replication and Treating COVID-19.
ACS Med Chem Lett 14: 1150-1151 (2023)
Smith, Gambrell & Russell
PARP7 Inhibition: A Promising Pathway to Advancements in Cancer Therapy.
ACS Med Chem Lett 14: 1141-1143 (2023)
Usona Institute
Discovery of Selective Tertiary Amide Inhibitors of Cyclin-Dependent Kinase 2 (CDK2).
ACS Med Chem Lett 14: 1179-1187 (2023)
Genentech
Novel Compounds as TEAD Inhibitors for Treating Cancer.
ACS Med Chem Lett 14: 1152-1153 (2023)
Smith, Gambrell & Russell
Discovery of Novel, Thienopyridine-Based Tyrosine Kinase Inhibitors Targeting Tumorigenic RON Splice Variants.
ACS Med Chem Lett 14: 1198-1207 (2023)
Wellmarkerbio Co.
New Horizons in Cancer Treatment: A Closer Look at Novel PI3Kα Inhibitors.
ACS Med Chem Lett 14: 1138-1140 (2023)
Usona Institute
Novel Haloacethydrazides as AEP Inhibitors for Treating Alzheimer's Disease.
ACS Med Chem Lett 14: 1165-1166 (2023)
Smith, Gambrell & Russell
Design and Synthesis of 1,3,5-Triazines or Pyrimidines Containing Dithiocarbamate Moiety as PI3Kα Selective Inhibitors.
ACS Med Chem Lett 14: 1266-1274 (2023)
Shenyang Pharmaceutical University
Discovery of
ACS Med Chem Lett 14: 1257-1265 (2023)
Peking Union Medical College
Brain-penetrant cyanoindane and cyanotetralin inhibitors of G2019S-LRRK2 kinase activity.
Bioorg Med Chem Lett 95: (2023)
Escape Bio
Galantamine-memantine hybrids for Alzheimer's disease: The influence of linker rigidity in biological activity and pharmacokinetic properties.
NA
Alma Mater Studiorum - University of Bologna
design of a stapled peptide targeting SARS-CoV-2 spike protein receptor-binding domain.
RSC Med Chem 14: 1722-1733 (2023)
Kansas State University
Design, synthesis, and biological evaluation of novel pyrimidin-2-amine derivatives as potent PLK4 inhibitors.
RSC Med Chem 14: 1787-1802 (2023)
Shenyang Pharmaceutical University
Discovery and computational studies of piperidine/piperazine-based compounds endowed with sigma receptor affinity.
RSC Med Chem 14: 1734-1742 (2023)
University of Messina
Research progress of anticancer drugs targeting CDK12.
RSC Med Chem 14: 1629-1644 (2023)
Qilu University of Technology
Enhancing allosteric inhibition of dihydrodipicolinate synthase through the design and synthesis of novel dimeric compounds.
RSC Med Chem 14: 1698-1703 (2023)
La Trobe University
Chloroacetamide fragment library screening identifies new scaffolds for covalent inhibition of the TEAD·YAP1 interaction.
RSC Med Chem 14: 1803-1816 (2023)
Indiana University School of Medicine 635 Barnhill Drive
Dual FLT3/haspin kinase inhibitor based on 3
RSC Med Chem 14: 1743-1754 (2023)
Purdue University
Discovery of rigid biphenyl
RSC Med Chem 14: 1755-1766 (2023)
National Center for Genetic Engineering and Biotechnology (BIOTEC)
Synthesis and biological evaluation of fluoroquinolones containing a pyridoxine derivatives moiety.
NA
Kazan (Volga region) Federal University
Regulation of Eukaryotic Translation Initiation Factor 4E as a Potential Anticancer Strategy.
J Med Chem 66: 12678-12696 (2023)
Qingdao University of Science and Technology
Design and synthesis of sulfonamides incorporating a biotin moiety: Carbonic anhydrase inhibitory effects, antiproliferative activity and molecular modeling studies.
Bioorg Med Chem 94: (2023)
University of Florence
Unraveling the unexpected aggregation behavior of Pyrazole-Based compounds Targeting Mycobacterium tuberculosis UDP-Galactopyranose mutase.
Bioorg Med Chem 94: (2023)
University of Saskatchewan
Targeting protein kinases for the treatment of Alzheimer's disease: Recent progress and future perspectives.
NA
Southwest Jiaotong University
Highly Selective Inhibitors of Dipeptidyl Peptidase 9 (DPP9) Derived from the Clinically Used DPP4-Inhibitor Vildagliptin.
J Med Chem 66: 12717-12738 (2023)
University of Antwerp
Discovery of 1,2-diaryl-3-oxopyrazolidin-4-carboxamides as a new class of MurA enzyme inhibitors and characterization of their antibacterial activity.
NA
German University in Cairo
Fragment-based and structure-guided discovery of perforin inhibitors.
Eur J Med Chem 261: (2023)
University of Auckland
Discovery of a non-covalent ligand for Rpn-13, a therapeutic target for hematological cancers.
Bioorg Med Chem Lett 95: (2023)
Purdue University
Applications of oxetanes in drug discovery and medicinal chemistry.
NA
University of Michigan
Progress in the development of TRPV1 small-molecule antagonists: Novel Strategies for pain management.
NA
Hospital of Chengdu University of Traditional Chinese Medicine
Synthesis and mechanism of action of new purine derivatives against triple negative breast cancer.
NA
Tianjin University of Science and Technology
Technologies of targeting histone deacetylase in drug discovery: Current progress and emerging prospects.
NA
Sichuan University
The latest perspectives of small molecules FMS kinase inhibitors.
NA
University of Sharjah
Truxillic acid monoamides as fatty acid binding protein 5 inhibitors.
Bioorg Med Chem 94: (2023)
Stony Brook University
Expanding the Structural Diversity at the Phenylene Core of Ligands for the von Hippel-Lindau E3 Ubiquitin Ligase: Development of Highly Potent Hypoxia-Inducible Factor-1α Stabilizers.
J Med Chem 66: 12776-12811 (2023)
University of Bonn
Structure-Based Drug Design of Novel Triaminotriazine Derivatives as Orally Bioavailable IDH2
J Med Chem 66: 12894-12910 (2023)
Nanjing University of Chinese Medicine
Rational Design of Sulfonyl-γ-AApeptides as Highly Potent HIV-1 Fusion Inhibitors with Broad-Spectrum Activity.
J Med Chem 66: 13319-13331 (2023)
University of South Florida
Design, Synthesis, and Activity Evaluation of Novel Dual-Target Inhibitors with Antifungal and Immunoregulatory Properties.
J Med Chem 66: 13007-13027 (2023)
Liaocheng University
Potent and selective carbonic anhydrase inhibition activities of pyrazolones bearing benzenesulfonamides.
Bioorg Med Chem Lett 95: (2023)
Adiyaman University
GNE-235: A Lead Compound Selective for the Second Bromodomain of PBRM1.
J Med Chem 66: 13116-13134 (2023)
Genentech
Exploration and Biological Evaluation of 1,3-Diamino-7
J Med Chem 66: 13946-13967 (2023)
Chinese Academy of Medical Sciences&Peking Union Medical College
Discovery of a First-in-Class CD38 Inhibitor for the Treatment of Mitochondrial Myopathy.
J Med Chem 66: 12762-12775 (2023)
Immunophage Biotech Co.
Novel Sulfonylurea-Based NLRP3 Inflammasome Inhibitor for Efficient Treatment of Nonalcoholic Steatohepatitis, Endotoxic Shock, and Colitis.
J Med Chem 66: 12966-12989 (2023)
Ocean University of China
Recent advances in small molecule and peptide inhibitors of glucose-regulated protein 78 for cancer therapy.
NA
The First Affiliated Hospital of Henan University
Discovery of marine phidianidine-based Nrf2 activators and their potential against oxLDL- and HG-induced injury in HUVECs.
Bioorg Med Chem Lett 95: (2023)
University of Jinan
Discovery of novel indazole derivatives as SOS1 agonists that activate KRAS signaling.
Bioorg Med Chem 93: (2023)
Sun Yat-Sen University
Identification of 1,3,4-oxadiazolyl-containing β-carboline derivatives as novel α-glucosidase inhibitors with antidiabetic activity.
NA
Wuyi University
Synthesis of bitopic ligands based on fallypride and evaluation of their affinity and selectivity towards dopamine D2 and D3 receptors.
NA
University of Pennsylvania
Reprogramming Energy Metabolism with Synthesized PDK Inhibitors Based on Dichloroacetate Derivatives and Targeted Delivery Systems for Enhanced Cancer Therapy.
J Med Chem 66: 14683-14699 (2023)
Wuhan University
Discovery of a novel series of medium-sized cyclic enteropeptidase inhibitors.
Bioorg Med Chem 93: (2023)
Takeda Pharmaceutical
Emerging opportunities to treat idiopathic pulmonary fibrosis: Design, discovery, and optimizations of small-molecule drugs targeting fibrogenic pathways.
NA
Institute of Respiratory Health
Discovery of Pyrazolo[1,5-a]pyrimidine derivative as a potent and selective PI3Kγ/δ dual inhibitor.
NA
Chinese Academy of Sciences
Discovery of anti-inflammatory natural flavonoids: Diverse scaffolds and promising leads for drug discovery.
NA
Hangzhou Normal University
Discovery of ARD-1676 as a Highly Potent and Orally Efficacious AR PROTAC Degrader with a Broad Activity against AR Mutants for the Treatment of AR + Human Prostate Cancer.
J Med Chem 66: 13280-13303 (2023)
University of Michigan
Discovery of Triazolyl Derivatives of Cucurbitacin B Targeting IGF2BP1 against Non-Small Cell Lung Cancer.
J Med Chem 66: 12931-12949 (2023)
Yanbian University
Discovery of a novel series of potent carbonic anhydrase inhibitors with selective affinity for μ Opioid receptor for Safer and long-lasting analgesia.
NA
University of Florence
Discovery of novel benzofuran-based derivatives as acetylcholinesterase inhibitors for the treatment of Alzheimer's disease: Design, synthesis, biological evaluation, molecular docking and 3D-QSAR investigation.
NA
National Research Centre
Oxetanes in Drug Discovery Campaigns.
J Med Chem 66: 12697-12709 (2023)
Imperial College London
Structure-Based Optimization of the Third Generation Type II Macrocycle TRK Inhibitors with Improved Activity against Solvent-Front, xDFG, and Gatekeeper Mutations.
J Med Chem 66: 12950-12965 (2023)
Jinan University
Discovery and Crystallography Study of Novel Biphenyl Ether and Oxadiazole Thioether (Non-Arylmethylamine)-Based Small-Molecule PD-1/PD-L1 Inhibitors as Immunotherapeutic Agents.
J Med Chem 66: 13172-13188 (2023)
Southern Medical University
Anti-influenza virus activities and mechanism of antrafenine analogs.
NA
The Chinese University of Hong Kong
Discovery of NLRP3 inhibitors using machine learning: Identification of a hit compound to treat NLRP3 activation-driven diseases.
NA
Peking University
Discovery of novel flavonoid-based CDK9 degraders for prostate cancer treatment via a PROTAC strategy.
NA
China Pharmaceutical University
Degradation of Cyclin-Dependent Kinase 9/Cyclin T1 by Optimized Microtubule-Associated Protein 1 Light Chain 3 Beta-Recruiting Coumarin Analogs.
J Med Chem 66: 12877-12893 (2023)
Shanghai Institute of Materia Medica
Discovery of three-dimensional bicyclo[3.3.1]nonanols as novel heat shock protein 90 inhibitors.
Bioorg Med Chem 93: (2023)
Tokyo Institute of Innovative Research
MNK, mTOR or eIF4E-selecting the best anti-tumor target for blocking translation initiation.
NA
Shandong University
Structural Mechanism and Inhibitors Targeting EGFR Exon 20 Insertion (Ex20ins) Mutations.
J Med Chem 66: 11656-11671 (2023)
Jinan University
Structure-Based Ligand Discovery Targeting the Transmembrane Domain of Frizzled Receptor FZD7.
J Med Chem 66: 11855-11868 (2023)
Shanghaitech University
Design and Preclinical Characterization Program toward Asundexian (BAY 2433334), an Oral Factor XIa Inhibitor for the Prevention and Treatment of Thromboembolic Disorders.
J Med Chem 66: 12203-12224 (2023)
Bayer
Design, synthesis and biological evaluation of pyrimidine base hydroxamic acid derivatives as dual JMJD3 and HDAC inhibitors.
Bioorg Med Chem Lett 94: (2023)
Tsinghua University
Tetrahydro-β-carboline derivatives as potent histone deacetylase 6 inhibitors with broad-spectrum antiproliferative activity.
NA
Northwest A&F University
Structure-based lead optimization to improve potency and selectivity of a novel tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid series of heparanase-1 inhibitor.
Bioorg Med Chem 93: (2023)
Taisho Pharmaceutical
Selective HDAC3 Inhibitors with Potent In Vivo Antitumor Efficacy against Triple-Negative Breast Cancer.
J Med Chem 66: 12033-12058 (2023)
Birla Institute of Technology and Science-Pilani Hyderabad
Discovery of a potent, orally available tricyclic derivative as a novel BRD4 inhibitor for melanoma.
Bioorg Med Chem 93: (2023)
Maruho Co.
Isolation and biological activity of natural chalcones based on antibacterial mechanism classification.
Bioorg Med Chem 93: (2023)
Shandong University of Technology
Rational discovery of dual FLT3/HDAC inhibitors as a potential AML therapy.
NA
Southern Medical University
Structure and function of SARS-CoV and SARS-CoV-2 main proteases and their inhibition: A comprehensive review.
NA
Baylor College of Medicine
Synthesis of cannabidiol-based compounds as ACE2 inhibitors with potential application in the treatment of COVID-19.
NA
Universidade Federal de Minas Gerais
Hydrophobicity modulation via the substituents at positions 2 and 4 of 1,3,5-triazine to enhance therapeutic ability against Alzheimer's disease for potent serotonin 5-HT6R agents.
NA
Jagiellonian University
Computational methods to analyze and predict the binding mode of inhibitors targeting both human and mushroom tyrosinase.
NA
University of Messina
A review: FDA-approved fluorine-containing small molecules from 2015 to 2022.
NA
Iran University of Medical Sciences
Targeted Degradation of Alpha-Synuclein by Autophagosome-Anchoring Chimera Peptides.
J Med Chem 66: 12614-12628 (2023)
Sun Yat-Sen University
Synthesis and biological evaluation of xanthine derivatives with phenacyl group as tryptophan hydroxylase 1 (TPH1) inhibitors for obesity and fatty liver disease.
Bioorg Med Chem Lett 94: (2023)
Gwangju Institute of Science and Technology
Discovery of (S)-N
Bioorg Med Chem Lett 94: (2023)
Zhejiang Chinese Medical University
Design, synthesis and bioevaluation of PI3Kα-selective inhibitors as potential colorectal cancer drugs.
NA
Guizhou Medical University
Design, synthesis and evaluation of novel pyrimidinylaminothiophene derivatives as FGFR1 inhibitors against human glioblastoma multiforme.
NA
Guangdong University of Technology
Discovery of N-(2-oxoethyl) sulfanilamide-derived inhibitors of KAT6A (MOZ) against leukemia by an isostere strategy.
NA
Children's Hospital Affiliated to Zhengzhou University
Micafungin: A promising inhibitor of UBE2M in cancer cell growth suppression.
NA
Zhengzhou University
Elemental exchange: Bioisosteric replacement of phosphorus by boron in drug design.
NA
Nathalal Parekh Marg
Synthesis of 1,3,5-triphenyl-1,2,4-triazole derivatives and their neuroprotection by anti-oxidative stress and anti-inflammation and protecting BBB.
NA
Sun Yat-sen University
Evolution of Slow-Binding Inhibitors Targeting Histone Deacetylase Isoforms.
J Med Chem 66: 11672-11700 (2023)
Osaka University
NADPH Oxidases: From Molecular Mechanisms to Current Inhibitors.
J Med Chem 66: 11632-11655 (2023)
TBA
Design, synthesis, and biological evaluation of novel HDAC/CD13 dual inhibitors for the treatment of cancer.
NA
Ocean University of China
Development of Long-Acting Dipeptidyl Peptidase-4 Inhibitors: Structural Evolution and Long-Acting Determinants.
J Med Chem 66: 11593-11631 (2023)
Sichuan Normal University
Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.
J Med Chem 66: 12141-12162 (2023)
High Point University
Design, synthesis and biological evaluation of 2,4,6- trisubstituted triazine derivatives as new nonpeptide small-molecule SIRT5 inhibitors.
Bioorg Med Chem 93: (2023)
Xihua University
Discovery of the Diphenyl 6-Oxo-1,6-dihydropyridazine-3-carboxylate/carboxamide Analogue J27 for the Treatment of Acute Lung Injury and Sepsis by Targeting JNK2 and Inhibiting the JNK2-NF-κB/MAPK Pathway.
J Med Chem 66: 12304-12323 (2023)
Wenzhou Medical University
Medicinal chemistry strategies targeting NLRP3 inflammasome pathway: A recent update from 2019 to mid-2023.
NA
Shenyang Pharmaceutical University
Discovery of a photosensitizing PI3K inhibitor for tumor therapy: Design, synthesis and in vitro biological evaluation.
Bioorg Med Chem Lett 94: (2023)
Fudan University
Identification of covalent fragment inhibitors for Plasmodium falciparum UCHL3 with anti-malarial efficacy.
Bioorg Med Chem Lett 94: (2023)
Purdue University
Synthesis and biological evaluation of simplified ajudazol derivatives reveal potent 5-lipoxygenase inhibition and considerable apoptotic activity in neuroblastoma cells.
Bioorg Med Chem Lett 94: (2023)
University Bonn
Discovery of antiviral SARS-CoV-2 main protease inhibitors by structure-guided hit-to-lead optimization of carmofur.
NA
Gwangju Institute of Science and Technology
Discovery of potent pyrrolo-pyrimidine and purine HDAC inhibitors for the treatment of advanced prostate cancer.
NA
University of Modena and Reggio Emilia
Development of a Selective Peptide κ-Opioid Receptor Antagonist by Late-Stage Functionalization with Cysteine Staples.
J Med Chem 66: 11843-11854 (2023)
Medical University of Vienna
Discovery and Characterization of Moracin C as an Anti-Gouty Arthritis/Hyperuricemia Candidate by Docking-Based Virtual Screening and Pharmacological Evaluation.
J Nat Prod 86: 2091-2101 (2023)
Southern Medical University
SIRT1-dependent mitochondrial biogenesis supports therapeutic effects of 4-butyl-polyhydroxybenzophenone compounds against NAFLD.
NA
Shanxi Medical University
Discovery of X10g as a selective PROTAC degrader of Hsp90α protein for treating breast cancer.
NA
Fujian Medical University (FMU)
Discovery, Synthesis, and Evaluation of Novel Dual Inhibitors of a Vascular Endothelial Growth Factor Receptor and Poly(ADP-Ribose) Polymerase for BRCA Wild-Type Breast Cancer Therapy.
J Med Chem 66: 12069-12100 (2023)
Sichuan University
Bioactive Isoquinoline Alkaloids with Diverse Skeletons from
J Nat Prod 86: 2162-2170 (2023)
Tianjin University of Technology
Magic shotgun approach to anti-inflammatory pharmacotherapy: Synthesis of novel thienopyrimidine monomers/heterodimer as dual COX-2 and 15-LOX inhibitors endowed with potent antioxidant activity.
NA
Zagazig University
2-Substituted 1,5-benzothiazepine-based HDAC inhibitors exert anticancer activities on human solid and acute myeloid leukemia cell lines.
Bioorg Med Chem 93: (2023)
University of Salerno
Cannabinoformins: Designing Biguanide-Embedded, Orally Available, Peripherally Selective Cannabinoid-1 Receptor Antagonists for Metabolic Syndrome Disorders.
J Med Chem 66: 11985-12004 (2023)
National Institute On Alcohol Abuse and Alcoholism (NIAAA)
Novel Amphibian Bowman-Birk-Like Inhibitor with Antioxidant and Anticoagulant Effects Ameliorates Pancreatitis Symptoms in Mice.
J Med Chem 66: 11869-11880 (2023)
Southern Medical University
Cyclotheonellazoles D-I, Potent Elastase Inhibitory Thiazole-Containing Cyclic Peptides from
J Nat Prod 86: 2216-2227 (2023)
Griffith University
Design, Synthesis, and Biological Evaluation of Thioglucoside Analogues of Gliflozin as Potent New Gliflozin Drugs.
J Med Chem 66: 12536-12543 (2023)
Huazhong University of Science & Technology
Discovery of WLB-89462, a New Drug-like and Highly Selective σ
J Med Chem 66: 12499-12519 (2023)
Welab Barcelona
Hydrophobic tag-based protein degradation: Development, opportunity and challenge.
NA
China Pharmaceutical University
Discovery of Highly Selective and Orally Bioavailable PI3Kδ Inhibitors with Anti-Inflammatory Activity for Treatment of Acute Lung Injury.
J Med Chem 66: 11905-11926 (2023)
Zhejiang University
YCH1899, a Highly Effective Phthalazin-1(2
J Med Chem 66: 12284-12303 (2023)
Shanghai Institute of Materia Medica
Discovery of a First-in-Class Degrader for the Lipid Kinase PIKfyve.
J Med Chem 66: 12432-12445 (2023)
Chinese Academy of Sciences
Structure-Activity Relationship of Truncated 2,8-Disubstituted-Adenosine Derivatives as Dual A
J Med Chem 66: 12249-12265 (2023)
Seoul National University
Discovery of highly potent covalent SARS-CoV-2 3CLpro inhibitors bearing 2-sulfoxyl-1,3,4-oxadiazole scaffold for combating COVID-19.
NA
Shanghai University of Traditional Chinese Medicine
Exploring positions 6 and 7 of a quinazoline-based scaffold leads to changes in selectivity and potency towards RIPK2/3 kinases.
NA
Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences
Development of selective class I protein arginine methyltransferase inhibitors through fragment-based drug design approach.
NA
CSIR-Indian Institute of Chemical Biology (IICB)
Natural products as potential lead compounds to develop new antiviral drugs over the past decade.
NA
Nanjing University of Chinese Medicine
Novel 4-Arylindolines Containing a Pyrido[3,2-
J Med Chem 66: 11815-11830 (2023)
Shenyang Pharmaceutical University
Targeting autophagy with small-molecule activators for potential therapeutic purposes.
NA
Sichuan University
HIV-1 Integrase Inhibitor, Dihydroobionin B, and the Investigation of Its Extraordinary Specific Rotation.
J Nat Prod 86: 2139-2144 (2023)
Hirosaki University
Alkyne as a Latent Warhead to Covalently Target SARS-CoV-2 Main Protease.
J Med Chem 66: 12237-12248 (2023)
University of Southern California
Discovery of Aminoratjadone Derivatives as Potent Noncovalent CRM1 Inhibitors.
J Med Chem 66: 11940-11950 (2023)
Sichuan University
Discovery and Mechanism Study of SARS-CoV-2 3C-like Protease Inhibitors with a New Reactive Group.
J Med Chem 66: 12266-12283 (2023)
Shanghaitech University
Novel Benzimidazoles as Potent Small-Molecule Inhibitors and Degraders of V-Domain Ig Suppressor of T-Cell Activation (VISTA).
J Med Chem 66: 11881-11892 (2023)
China Pharmaceutical University
Discovery and Structural Optimization of Covalent ZAP-70 Kinase Inhibitors against Psoriasis.
J Med Chem 66: 12018-12032 (2023)
Shanghai Institute of Materia Medica
Discovery, Optimization, and Evaluation of Novel
J Med Chem 66: 12373-12395 (2023)
Chinese Academy of Medical Sciences & Peking Union Medical College
Antibacterial activities of anthraquinones: structure-activity relationships and action mechanisms.
RSC Med Chem 14: 1446-1471 (2023)
Shanghai Veterinary Research Institute
Discovery of imeglimin-inspired novel 1,3,5-triazine derivatives as antidiabetic agents in streptozotocin-induced diabetes in Wistar rats
RSC Med Chem 14: 1512-1536 (2023)
Sam Higginbottom University of Agriculture
Discovery of novel methionine adenosyltransferase 2A (MAT2A) allosteric inhibitors by structure-based virtual screening.
Bioorg Med Chem Lett 94: (2023)
Orion Pharma
Development of a highly potent and selective degrader of LRRK2.
Bioorg Med Chem Lett 94: (2023)
Harvard University
6-Azaspiro[2.5]octanes as small molecule agonists of the human glucagon-like peptide-1 receptor.
Bioorg Med Chem Lett 94: (2023)
Pfizer
Structure and ligand based design for identification of highly potent molecules against 5-LOX.
Bioorg Med Chem Lett 94: (2023)
Guru Nanak Dev University
Bicyclic Peptide Library Screening for the Identification of Gαi Protein Modulators.
J Med Chem 66: 12396-12406 (2023)
University of Bonn
Design, synthesis, antitumor activity, and molecular dynamics simulations of novel sphingosine kinase 2 inhibitors.
Bioorg Med Chem 93: (2023)
Hebei University
Kinetics, Thermodynamics, and Structural Effects of Quinoline-2-Carboxylates, Zinc-Binding Inhibitors of New Delhi Metallo-β-lactamase-1 Re-sensitizing Multidrug-Resistant Bacteria for Carbapenems.
J Med Chem 66: 11761-11791 (2023)
Freie University Berlin
Discovery of 2-Aminopyrimidine Derivatives as Potent Dual FLT3/CHK1 Inhibitors with Significantly Reduced hERG Inhibitory Activities.
J Med Chem 66: 11792-11814 (2023)
Zhejiang University
Identification of Novel Quinolin-2(1
J Med Chem 66: 12468-12478 (2023)
Sun Yat-Sen University
2B Determined: The Future of the Serotonin Receptor 2B in Drug Discovery.
J Med Chem 66: 11027-11039 (2023)
Vanderbilt University
Identification of Novel Dual-Target Estrogen Receptor α Degraders with Tubulin Inhibitory Activity for the Treatment of Endocrine-Resistant Breast Cancer.
J Med Chem 66: 11094-11117 (2023)
Zhongnan Hospital of Wuhan University
Novel Dihydroorotate Dehydrogenase Inhibitors for Treating Acute Myelogenous Leukemia.
ACS Med Chem Lett 14: 1043-1044 (2023)
Smith, Gambrell & Russell
Inhibition Profiles of Some Novel Sulfonamide-Incorporated α-Aminophosphonates on Human Carbonic Anhydrases.
ACS Med Chem Lett 14: 1067-1072 (2023)
Riga Technical University
Design, Construction, and Screening of Diversified Pyrimidine-Focused DNA-Encoded Libraries.
ACS Med Chem Lett 14: 1073-1078 (2023)
Nanjing University of Chinese Medicine
Discovery of a Novel Photocaged PI3K Inhibitor Capable of Real-Time Reporting of Drug Release.
ACS Med Chem Lett 14: 1100-1107 (2023)
Chinese Academy of Medical Sciences and Peking Union Medical College
Fused Pyrazole Urea Analogs as Glucosylceramide Synthase Inhibitors for Treating Diseases.
ACS Med Chem Lett 14: 1031-1032 (2023)
Smith, Gambrell & Russell
Structure-Activity Relationship Study of 1
ACS Med Chem Lett 14: 1079-1087 (2023)
University of Chinese Academy of Sciences
Discovery of
ACS Med Chem Lett 14: 1113-1121 (2023)
The Affiliated Hospital of Southwest Jiaotong University
Cyclin-Dependent Kinase Degradation via E3 Ligase Binding for Potential Disease Modulation in Cancer Treatment.
ACS Med Chem Lett 14: 1035-1037 (2023)
Usona Institute
Pyridazine Derivatives as NLRP3 Inhibitors for Treating Asthma, COPD, Parkinson's Disease, and Alzheimer's Disease.
ACS Med Chem Lett 14: 1047-1048 (2023)
Smith, Gambrell & Russell
Discovery of MK-8768, a Potent and Selective mGluR2 Negative Allosteric Modulator.
ACS Med Chem Lett 14: 1088-1094 (2023)
Merck
Discovery of the TLR7/8 Antagonist MHV370 for Treatment of Systemic Autoimmune Diseases.
ACS Med Chem Lett 14: 1054-1062 (2023)
Novartis Institutes for Biomedical Research
Structure-Based Design of Transport-Specific Multitargeted One-Carbon Metabolism Inhibitors in Cytosol and Mitochondria.
J Med Chem 66: 11294-11323 (2023)
Duquesne University
Design, Synthesis, and Biological Evaluation of Novel P2X7 Receptor Antagonists for the Treatment of Septic Acute Kidney Injury.
J Med Chem 66: 11365-11389 (2023)
Sichuan University
Indazole as a Phenol Bioisostere: Structure-Affinity Relationships of GluN2B-Selective NMDA Receptor Antagonists.
J Med Chem 66: 11573-11588 (2023)
University Munster
Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2).
J Med Chem 66: 10991-11026 (2023)
University of Texas Medical Branch (UTMB)
Progress on the Pharmacological Targeting of Janus Pseudokinases.
J Med Chem 66: 10959-10990 (2023)
Yale University
Tetrazole and oxadiazole derivatives as bioisosteres of tariquidar and elacridar: New potent P-gp modulators acting as MDR reversers.
NA
University of Florence
Small molecule inhibitors of NLRP3 inflammasome and GSK-3β in the management of traumatic brain injury: A review.
NA
National Institute of Pharmaceutical Education and Research (NIPER)
Discovery and structure-activity relationships (SAR) of a novel class of 2-substituted N-piperidinyl indole-based nociceptin opioid receptor ligands.
Bioorg Med Chem 92: (2023)
Astraea Therapeutics
A TNF-α blocking peptide that reduces NF-κB and MAPK activity for attenuating inflammation.
Bioorg Med Chem 92: (2023)
Changchun University of Science and Technology
Design and optimization of selective and potent CDK9 inhibitors with flavonoid scaffold for the treatment of acute myeloid leukemia.
NA
China Pharmaceutical University
Discovery and optimization of 2,3-diaryl-1,3-thiazolidin-4-one-based derivatives as potent and selective cytotoxic agents with anti-inflammatory activity.
NA
Umm Al-Qura University
Synthesis, computational and experimental pharmacological studies for (thio)ether-triazine 5-HT6R ligands with noticeable action on AChE/BChE and chalcogen-dependent intrinsic activity in search for new class of drugs against Alzheimer's disease.
NA
Jagiellonian University
Vinylphosphonate-based cyclic dinucleotides enhance STING-mediated cancer immunotherapy.
NA
Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences
Identification of [1,2,4]Triazolo[4,3-a]pyrazine PARP1 inhibitors with overcome acquired resistance activities.
NA
Shanghai Jiao Tong University
Discovery of Small-Molecule TIM-3 Inhibitors for Acute Myeloid Leukemia Using Pharmacophore-Based Virtual Screening.
J Med Chem 66: 11464-11475 (2023)
Weill Cornell Medicine
Discovery of chiral 1,4-diarylazetidin-2-one-based hydroxamic acid derivatives as novel tubulin polymerization inhibitors with histone deacetylase inhibitory activity.
Bioorg Med Chem 92: (2023)
Fudan University
Structure activity relationships of 5-HT2B and 5-HT2C serotonin receptor antagonists: N6, C2 and 5'-Modified (N)-methanocarba-adenosine derivatives.
NA
National Institute of Diabetes and Digestive and Kidney Diseases
A Systematic Survey of Reversibly Covalent Dipeptidyl Inhibitors of the SARS-CoV-2 Main Protease.
J Med Chem 66: 11040-11055 (2023)
Texas A&M University
Identification of a Protein Arginine Methyltransferase 7 (PRMT7)/Protein Arginine Methyltransferase 9 (PRMT9) Inhibitor.
J Med Chem 66: 13665-13683 (2023)
University of Salerno
Design, synthesis, and biological evaluation of 1,6-naphthyridine-2-one derivatives as novel FGFR4 inhibitors for the treatment of colorectal cancer.
NA
Wenzhou Medical University
Triazole hybrid compounds: A new frontier in malaria treatment.
NA
Universiti Kebangsaan Malaysia (UKM)
Discovery of indolinone-bearing benzenesulfonamides as new dual carbonic anhydrase and VEGFR-2 inhibitors possessing anticancer and pro-apoptotic properties.
NA
Kafrelsheikh University
Structure Guided Design, Synthesis, and Biological Evaluation of Oxetane-Containing Indole Analogues.
Bioorg Med Chem 92: (2023)
Baylor University
Discovery of 2,4-diphenyl-substituted thiazole derivatives as PRMT1 inhibitors and investigation of their anti-cervical cancer effects.
Bioorg Med Chem 92: (2023)
Minzu University of China
Structure-Activity Relationship Studies of 2,4,5-Trisubstituted Pyrimidine Derivatives Leading to the Identification of a Novel and Potent Sirtuin 5 Inhibitor against Sepsis-Associated Acute Kidney Injury.
J Med Chem 66: 11517-11535 (2023)
Xihua University
Rational Design and Development of Selective BRD7 Bromodomain Inhibitors and Their Activity in Prostate Cancer.
J Med Chem 66: 11250-11270 (2023)
Purdue University
Design, Synthesis, and Anti-Inflammatory Evaluation of a Novel PPARδ Agonist with a 4-(1-Pyrrolidinyl)piperidine Structure.
J Med Chem 66: 11428-11446 (2023)
Shionogi
Facilitated Drug Repurposing with Artemisinin-Derived PROTACs: Unveiling PCLAF as a Therapeutic Target.
J Med Chem 66: 11335-11350 (2023)
Guizhou Medical University
Discovery, SAR Study of GST Inhibitors from a Novel Quinazolin-4(1
J Med Chem 66: 11118-11132 (2023)
Chinese Academy of Sciences
Synthesis and anti-cancer potential of potent peripheral MAOA inhibitors designed to limit blood:brain penetration.
Bioorg Med Chem 92: (2023)
University of Southern California
Targeting polyketide synthase 13 for the treatment of tuberculosis.
NA
China Pharmaceutical University
Design, synthesis, and biological evaluation of 3, 5-disubsituted-1H-pyrazolo[3,4-b]pyridines as multiacting inhibitors against microtubule and kinases.
NA
Southern University of Science and Technology
Thiazole-based analogues as potential antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA) and their SAR elucidation.
NA
Jiangxi Science & Technology Normal University
Recent advances in the development of inhibitors targeting KRAS-G12C and its related pathways.
NA
Tianjin University of Science & Technology
Novel acridine-based LSD1 inhibitors enhance immune response in gastric cancer.
NA
Zhenzhou University
Current development of 1,2,3-triazole derived potential antimalarial scaffolds: Structure- activity relationship (SAR) and bioactive compounds.
NA
Central University of Punjab
Glycogen synthase kinase-3: A potential target for diabetes.
Bioorg Med Chem 92: (2023)
L. M. College of Pharmacy
An overview of phosphodiesterase 9 inhibitors: Insights from skeletal structure, pharmacophores, and therapeutic potential.
NA
Southern Medical University
Neutral sphingomyelinase 2 inhibitors based on the pyrazolo[1,5-a]pyrimidin-3-amine scaffold.
NA
Academy of Sciences of the Czech Republic V.v.i.
5-Cyano substituted diarylpyridines as potent HIV-1 NNRTIs: Rational design, synthesis, and activity evaluation.
NA
Shandong University
Discovery of AD258 as a Sigma Receptor Ligand with Potent Antiallodynic Activity.
J Med Chem 66: 11447-11463 (2023)
Universit£
PROTACs Targeting MLKL Protect Cells from Necroptosis.
J Med Chem 66: 11216-11236 (2023)
Pharmaxis
Inhibition of FLT3-ITD Kinase in Acute Myeloid Leukemia by New Imidazo[1,2-
J Med Chem 66: 11133-11157 (2023)
Institute of Organic Chemistry and Biochemistry of The Czech Academy of Sciences
Small-Molecule Hydrophobic Tagging: A Promising Strategy of Druglike Technology for Targeted Protein Degradation.
J Med Chem 66: 10917-10933 (2023)
China Pharmaceutical University
Discovery of quinazoline HPK1 inhibitors with high cellular potency.
Bioorg Med Chem 92: (2023)
Emd Serono Research & Development Institute
RIPK2 inhibitors for disease therapy: Current status and perspectives.
NA
Sichuan University
Cannabidiol Analogue
J Med Chem 66: 11498-11516 (2023)
University of Science and Technology of China
5-Substituted Pyridine-2,4-dicarboxylate Derivatives Have Potential for Selective Inhibition of Human Jumonji-C Domain-Containing Protein 5.
J Med Chem 66: 10849-10865 (2023)
University of Oxford
Flindissone, a Limonoid Isolated from
J Nat Prod 86: 1901-1909 (2023)
University of Vienna
Design, Synthesis, and Application of Fluorescent Ligands Targeting the Intracellular Allosteric Binding Site of the CXC Chemokine Receptor 2.
J Med Chem 66: 12911-12930 (2023)
University of Nottingham Biodiscovery Institute
Structure-Activity Relationship Studies on Cell-Potent Nicotinamide
J Med Chem 66: 10510-10527 (2023)
Purdue University
Discovery of SMD-3040 as a Potent and Selective SMARCA2 PROTAC Degrader with Strong
J Med Chem 66: 10761-10781 (2023)
University of Michigan
Discovery and structure-activity relationship studies of novel α-ketoamide derivatives targeting the SARS-CoV-2 main protease.
NA
Sichuan University
Suramin analogues protect cartilage against osteoarthritic breakdown by increasing levels of tissue inhibitor of metalloproteinases 3 (TIMP-3) in the tissue.
Bioorg Med Chem 92: (2023)
University of East Anglia
Discovery of triazole-bridged aryl adamantane analogs as an intriguing class of multifunctional agents for treatment of Alzheimer's disease.
NA
Indian Institute of Technology (Banaras Hindu University)
The mystery of titan hunter: Rationalized striking of the MAPK pathway via Newly synthesized 6-Indolylpyridone-3-Carbonitrile derivatives.
NA
Tanta University
Creation of a Peptide Antagonist of the GFRAL-RET Receptor Complex for the Treatment of GDF15-Induced Malaise.
J Med Chem 66: 11237-11249 (2023)
University of Pennsylvania
Macrocyclic Peptidomimetic Plasmepsin X Inhibitors with Potent
J Med Chem 66: 10658-10680 (2023)
Latvian Institute of Organic Synthesis
1,5-Diaryl-1,2,4-triazole Ureas as New SLC-0111 Analogues Endowed with Dual Carbonic Anhydrase and VEGFR-2 Inhibitory Activities.
J Med Chem 66: 10558-10578 (2023)
Kafrelsheikh University
Cell-active, irreversible covalent inhibitors that selectively target the catalytic lysine of EGFR by using fluorosulfate-based SuFEx chemistry.
NA
National University of Singapore
Development of novel celastrol-ligustrazine hybrids as potent peroxiredoxin 1 inhibitors against lung cancer.
NA
Anhui University of Science and Technology
AI-Powered Virtual Screening of Large Compound Libraries Leads to the Discovery of Novel Inhibitors of Sirtuin-1.
J Med Chem 66: 10241-10251 (2023)
Enamine
Discovery and Characterization of a Chemical Probe Targeting the Zinc-Finger Ubiquitin-Binding Domain of HDAC6.
J Med Chem 66: 10273-10288 (2023)
University of Toronto
Discovery of Novel 1,2,3,4-Tetrahydrobenzofuro[2,3-
J Med Chem 66: 10791-10807 (2023)
Zhejiang University
Design, Synthesis, and Antitumor Activity Evaluation of 2-Arylmethoxy-4-(2,2'-dihalogen-substituted biphenyl-3-ylmethoxy) Benzylamine Derivatives as Potent PD-1/PD-L1 Inhibitors.
J Med Chem 66: 10579-10603 (2023)
Zhejiang University
Identification of Pyrido[3,4-d]pyrimidine derivatives as RIPK3-Mediated necroptosis inhibitors.
NA
Korea University
Design, synthesis and biological evaluation of salicylanilides as novel allosteric inhibitors of human pancreatic lipase.
Bioorg Med Chem 91: (2023)
Shanghai University of Traditional Chinese Medicine
Exploitation of Proximity-Mediated Effects in Drug Discovery: An Update of Recent Research Highlights in Perturbing Pathogenic Proteins and Correlated Issues.
J Med Chem 66: 10122-10149 (2023)
Anhui University of Chinese Medicine
Principles and Applications of CF
J Med Chem 66: 10202-10225 (2023)
Eberhard Karls Universit£T T£Bingen
Leucettinibs, a Class of DYRK/CLK Kinase Inhibitors Inspired by the Marine Sponge Natural Product Leucettamine B.
J Med Chem 66: 10694-10714 (2023)
Perha Pharmaceuticals
Quinolinetrione-tacrine hybrids as multi-target-directed ligands against Alzheimer's disease.
Bioorg Med Chem 91: (2023)
Alma Mater Studiorum - University of Bologna
Catechol-mimicking transition-state analogues as non-oxidizable inhibitors of tyrosinases.
NA
Univ. Grenoble Alpes
A review of progress in o-aminobenzamide-based HDAC inhibitors with dual targeting capabilities for cancer therapy.
NA
Zhengzhou University
Discovery and Optimization of a STING Agonist Platform for Application in Antibody Drug Conjugates.
J Med Chem 66: 10715-10733 (2023)
Mersana Therapeutics
Design, synthesis, and mechanistic study of 2-piperazineone-bearing peptidomimetics as novel HIV capsid modulators.
RSC Med Chem 14: 1272-1295 (2023)
Shandong University
Hypoxia-activated prodrugs of phenolic olaparib analogues for tumour-selective chemosensitisation.
RSC Med Chem 14: 1309-1330 (2023)
University of Auckland
Synthesis and pharmacological evaluation of 1,3-diaryl substituted pyrazole based (thio)urea derivatives as potent antimicrobial agents against multi-drug resistant
RSC Med Chem 14: 1296-1308 (2023)
National Institute of Pharmaceutical Education and Research (NIPER)
Novel 1,2,4-oxadiazole compounds as PPAR-α ligand agonists: a new strategy for the design of antitumour compounds.
RSC Med Chem 14: 1377-1388 (2023)
Universidad Complutense of Madrid
Research and development of
RSC Med Chem 14: 1209-1226 (2023)
University of South China
Is structural hybridization invoking new dimensions for antimalarial drug discovery research?
RSC Med Chem 14: 1227-1253 (2023)
University of Delhi
Novel fused imidazotriazines acting as promising top. II inhibitors and apoptotic inducers with greater selectivity against head and neck tumors: Design, synthesis, and biological assessments.
NA
Ahram Canadian University
Discovery of new diaryl ether inhibitors against Mycobacterium tuberculosis targeting the minor portal of InhA.
NA
Universita Toulouse III - Paul Sabatier (UT3)
Exploring diverse reactive warheads for the design of SARS-CoV-2 main protease inhibitors.
NA
The State University of New Jersey
Recent advances in triazoles as tyrosinase inhibitors.
NA
University of Health Sciences
Synthesis, cytotoxicity, antioxidant activity and molecular modeling of new NSAIDs-EBS derivatives.
NA
Jianghan University
Metabolism-guided development of Ko143 analogs as ABCG2 inhibitors.
NA
University of Pittsburgh
Strategies of targeting CYP51 for IFIs therapy: Emerging prospects, opportunities and challenges.
NA
Sichuan University
PepScaf: Harnessing Machine Learning with In Vitro Selection toward De Novo Macrocyclic Peptides against IL-17C/IL-17RE Interaction.
J Med Chem 66: 11187-11200 (2023)
Zhejiang University
Discovery of Novel d-(+)-Biotin-Conjugated Resorcinol Dibenzyl Ether-Based PD-L1 Inhibitors for Targeted Cancer Immunotherapy.
J Med Chem 66: 10364-10380 (2023)
Zunyi Medical University
Synthesis and activity of β-carboline antimalarials targeting the Plasmodium falciparum heat shock 90 protein.
Bioorg Med Chem Lett 92: (2023)
California Polytechnic State University
Discovery of a novel dual-target inhibitor of CDK12 and PARP1 that induces synthetic lethality for treatment of triple-negative breast cancer.
NA
Southwest Jiaotong University
Synthesis and antibacterial activities of baulamycin A inspired derivatives.
NA
Korea University
Exploring the 1,3-benzoxazine chemotype for cannabinoid receptor 2 as a promising anti-cancer therapeutic.
NA
University of the Studies of Bari "Aldo Moro"
Coumarins as factor XIIa inhibitors: Potency and selectivity improvements using a fragment-based strategy.
NA
University of Namur
Discovery of a Bromodomain and Extra Terminal Domain (BET) Inhibitor with the Selectivity for the Second Bromodomain (BD2) and the Capacity for the Treatment of Inflammatory Diseases.
J Med Chem 66: 10824-10848 (2023)
China Pharmaceutical University
2-Substituted quinazolines: Partial agonistic and antagonistic ligands of the constitutive androstane receptor (CAR).
NA
Charles University
C-2 Thiophenyl Tryptophan Trimers Inhibit Cellular Entry of SARS-CoV-2 through Interaction with the Viral Spike (S) Protein.
J Med Chem 66: 10432-10457 (2023)
Instituto De Quimica Medica (IQM)
Design of Cell-Permeable Inhibitors of Eukaryotic Translation Initiation Factor 4E (eIF4E) for Inhibiting Aberrant Cap-Dependent Translation in Cancer.
J Med Chem 66: 10734-10745 (2023)
University of Michigan
Recent advance of small-molecule drugs for clinical treatment of osteoporosis: A review.
NA
Zhengzhou Normal University
Discovery of novel and selective SIK2 inhibitors by the application of AlphaFold structures and generative models.
Bioorg Med Chem 91: (2023)
Insilico Medicine Shanghai
Pharmacological and Physicochemical Properties Optimization for Dual-Target Dopamine D
J Med Chem 66: 10304-10341 (2023)
National Institute On Drug Abuse?Intramural Research Program
Macrocyclic Carbon-Linked Pyrazoles As Novel Inhibitors of MCL-1.
ACS Med Chem Lett 14: 955-961 (2023)
Janssen Research & Development
PptT Inhibitors Based on Heterocyclic Replacements of Amidinoureas.
ACS Med Chem Lett 14: 970-976 (2023)
University of North Carolina at Chapel Hill
-Alkyl Carbamoylimidazoles as Versatile Synthons for the Synthesis of Urea-Based PSMA Inhibitors.
ACS Med Chem Lett 14: 943-948 (2023)
University of Alberta
Development of Riluzole Analogs with Improved Use-Dependent Inhibition of Skeletal Muscle Sodium Channels.
ACS Med Chem Lett 14: 999-1008 (2023)
University of Bari Aldo Moro
The Hitchhiker's Guide to Deep Learning Driven Generative Chemistry.
ACS Med Chem Lett 14: 901-915 (2023)
Insilico Medicine Hong Kong
Discovery of New Binders for DCAF1, an Emerging Ligase Target in the Targeted Protein Degradation Field.
ACS Med Chem Lett 14: 949-954 (2023)
Novartis Institutes for Biomedical Research
Novel Lactams as CBL-B Inhibitors for Treating Cancer.
ACS Med Chem Lett 14: 897-898 (2023)
Smith, Gambrell & Russell
Novel Dihydroorotate Dehydrogenase Inhibitors for Treating Acute Myelogenous Leukemia.
ACS Med Chem Lett 14: 891-892 (2023)
Smith, Gambrell & Russell
Diselenide Covalent Allosteric Inhibitors of Glutaminase with Strong
ACS Med Chem Lett 14: 920-928 (2023)
Zhejiang University
Fused Bicyclic Heteroaryl Compounds as NLRP3 Inhibitors for Treating Asthma or COPD.
ACS Med Chem Lett 14: 895-896 (2023)
Smith, Gambrell & Russell
Discovery of Potent, Dual-Inhibitors of Diacylglycerol Kinases Alpha and Zeta Guided by Phenotypic Optimization.
ACS Med Chem Lett 14: 929-935 (2023)
Bristol Myers Squibb Research and Early Development
Optimization of 1,2,4-Triazole-Based p97 Inhibitors for the Treatment of Cancer.
ACS Med Chem Lett 14: 977-985 (2023)
University of Pittsburgh Chemical Diversity Center
Novel Diaminopyrimidine Carboxamides as HPK1 Inhibitors for Treating Cancer.
ACS Med Chem Lett 14: 899-900 (2023)
Smith, Gambrell & Russell
Discovery of a Series of Indane-Containing NBTIs with Activity against Multidrug-Resistant Gram-Negative Pathogens.
ACS Med Chem Lett 14: 993-998 (2023)
Roche Pharma Research & Early Development
Structure-Activity Relationships of Alanine Scan Mutants αO-Conotoxins GeXIVA[1,2] and GeXIVA[1,4].
J Med Chem 66: 10092-10107 (2023)
Guangxi University
Discovery of HDAC6, HDAC8, and 6/8 Inhibitors and Development of Cell-Based Drug Screening Models for the Treatment of TGF-β-Induced Idiopathic Pulmonary Fibrosis.
J Med Chem 66: 10528-10557 (2023)
National Taiwan University
Discovery of the First Irreversible HDAC6 Isoform Selective Inhibitor with Potent Anti-Multiple Myeloma Activity.
J Med Chem 66: 10080-10091 (2023)
Shandong University
Discovery of Novel Oleamide Analogues as Brain-Penetrant Positive Allosteric Serotonin 5-HT
J Med Chem 66: 9992-10009 (2023)
University of Texas Medical Branch (UTMB)
Synthesis and characterization of the N-succinyl-l,l-diaminopimelic acid desuccinylase (DapE) alternate substrate analog N,N-dimethyl-l,l-SDAP.
Bioorg Med Chem 91: (2023)
Loyola University Chicago
Discovery of a Novel Bifunctional Steroid Analog, YXG-158, as an Androgen Receptor Degrader and CYP17A1 Inhibitor for the Treatment of Enzalutamide-Resistant Prostate Cancer.
J Med Chem 66: 9972-9991 (2023)
Shanghai Institute of Materia Medica
Immunosuppressive effects of new thiophene-based KV1.3 inhibitors.
NA
University of Ljubljana
Optimizing metabolic stability of phosphodiesterase 5 inhibitors: Discovery of a potent N-(pyridin-3-ylmethyl)quinoline derivative targeting synaptic plasticity.
Bioorg Med Chem Lett 92: (2023)
Columbia University
Quinazoline-based VEGFR-2 inhibitors as potential anti-angiogenic agents: A contemporary perspective of SAR and molecular docking studies.
NA
Tehran University of Medical Sciences
Discovery of Novel Potent Covalent Glutathione Peroxidase 4 Inhibitors as Highly Selective Ferroptosis Inducers for the Treatment of Triple-Negative Breast Cancer.
J Med Chem 66: 10036-10059 (2023)
China Pharmaceutical University
Exploring Structural Determinants of Bias among D4 Subtype-Selective Dopamine Receptor Agonists.
J Med Chem 66: 9710-9730 (2023)
Friedrich-Alexander-Universitat Erlangen-Nurnberg
Cannabinoid Receptor Type II Ligands from Sandalwood Oil and Synthetic α-Santalol Derivatives.
J Nat Prod 86: 1786-1792 (2023)
University of Mississippi
Design, Synthesis, and Biological Evaluation of 2-Hydroxy-4-phenylthiophene-3-carbonitrile as PD-L1 Antagonist and Its Comparison to Available Small Molecular PD-L1 Inhibitors.
J Med Chem 66: 9577-9591 (2023)
University Medical Center Groningen
Discovery of BI 7446: A Potent Cyclic Dinucleotide STING Agonist with Broad-Spectrum Variant Activity for the Treatment of Cancer.
J Med Chem 66: 9376-9400 (2023)
Boehringer Ingelheim Pharma
Discovery and Characterization of PROTACs Targeting Tissue Transglutaminase (TG2).
J Med Chem 66: 9445-9465 (2023)
Northwestern University
Medicinal Chemistry Insights into the Development of Small-Molecule Kelch-Like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Protein-Protein Interaction Inhibitors.
J Med Chem 66: 9325-9344 (2023)
China Pharmaceutical University
Stereochemistry-Driven Interactions of α,γ-Peptide Ligands with the Neuropeptide Y Y
J Med Chem 66: 9642-9657 (2023)
University of Regensburg
Innovative Strategy toward Mutant CFTR Rescue in Cystic Fibrosis: Design and Synthesis of Thiadiazole Inhibitors of the E3 Ligase RNF5.
J Med Chem 66: 9797-9822 (2023)
University of Bologna
Novel 1,4-Dihydropyridines as Specific Binders and Activators of SIRT3 Impair Cell Viability and Clonogenicity and Downregulate Hypoxia-Induced Targets in Cancer Cells.
J Med Chem 66: 9622-9641 (2023)
Sapienza University of Rome
Discovery of Sulanemadlin (ALRN-6924), the First Cell-Permeating, Stabilized α-Helical Peptide in Clinical Development.
J Med Chem 66: 9401-9417 (2023)
Aileron Therapeutics
Discovery and Evaluation of 3-Quinoxalin Urea Derivatives as Potent, Selective, and Orally Available ATM Inhibitors Combined with Chemotherapy for the Treatment of Cancer via Goal-Oriented Molecule Generation and Virtual Screening.
J Med Chem 66: 9495-9518 (2023)
Sichuan University
Biological Function of Pin1 in Vivo and Its Inhibitors for Preclinical Study: Early Development, Current Strategies, and Future Directions.
J Med Chem 66: 9251-9277 (2023)
Shanghai University
Discovery of benzodiazepine derivatives as a new class of covalent inhibitors of SARS-CoV-2 main protease.
Bioorg Med Chem Lett 92: (2023)
Sichuan University
A dual nociceptin and mu opioid receptor agonist exhibited robust antinociceptive effect with decreased side effects.
NA
National Health Research Institutes
An overview of anti-SARS-CoV-2 and anti-inflammatory potential of baicalein and its metabolite baicalin: Insights into molecular mechanisms.
NA
Tripura University
2,4-Diaryl-pyrimido[1,2-a]benzimidazole derivatives as novel anticancer agents endowed with potent anti-leukemia activity: Synthesis, biological evaluation and kinase profiling.
NA
Kafrelsheikh University
Design, synthesis and biological evaluation of indazole derivatives as selective covalent inhibitors of FGFR4 in wild-type and gatekeeper mutants.
NA
Sichuan University
Discovery of novel thymidylate synthase (TS) inhibitors that influence cancer angiogenesis and metabolic reprogramming in NSCLC cells.
NA
China Medical University
Structure-Activity Relationship Study of Cannabidiol-Based Analogs as Negative Allosteric Modulators of the μ-Opioid Receptor.
J Med Chem 66: 9466-9494 (2023)
Indiana University
Discovery of IACS-52825, a Potent and Selective DLK Inhibitor for Treatment of Chemotherapy-Induced Peripheral Neuropathy.
J Med Chem 66: 9954-9971 (2023)
The University of Texas Md Anderson Cancer Center
First-in-Class Dual Targeting Compounds for the Management of Seizures in Glucose Transporter Type 1 Deficiency Syndrome.
J Med Chem 66: 10010-10026 (2023)
University of Florence
Potent, Selective, and Membrane Permeable 2-Amino-4-Substituted Pyridine-Based Neuronal Nitric Oxide Synthase Inhibitors.
J Med Chem 66: 9934-9953 (2023)
Northwestern University
Structure-Guided Chemical Optimization of Bicyclic Peptide (
J Med Chem 66: 9881-9893 (2023)
Bicycletx
Design and discovery of new selective and potent VEGF receptor 2 tyrosine kinase inhibitors.
Bioorg Med Chem 91: (2023)
Nankai University
Are inhibitors of histone deacetylase 8 (HDAC8) effective in hematological cancers especially acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL)?
NA
Jadavpur University
Discovery of tetrahydroisoquinolineindole derivatives as first dual PRMT5 inhibitors/hnRNP E1 upregulators: Design, synthesis and biological evaluation.
NA
University of Jinan
Aldo-Keto Reductase 1C3 Inhibitor Prodrug Improves Pharmacokinetic Profile and Demonstrates In Vivo Efficacy in a Prostate Cancer Xenograft Model.
J Med Chem 66: 9894-9915 (2023)
University of Nebraska Medical Center
Enantioselective Synthesis and Biological Evaluation of Pyrrolidines Bearing Quaternary Stereogenic Centers.
J Med Chem 66: 9866-9880 (2023)
Chongqing University
Opportunities and Challenges for Inhibitors Targeting Citrate Transport and Metabolism in Drug Discovery.
J Med Chem 66: 9229-9250 (2023)
China Pharmaceutical University
Discovery of a Potent and Selective Tyrosine Kinase 2 Inhibitor: TAK-279.
J Med Chem 66: 10473-10496 (2023)
Nimbus Therapeutics
Discovery of HPG1860, a Structurally Novel Nonbile Acid FXR Agonist Currently in Clinical Development for the Treatment of Nonalcoholic Steatohepatitis.
J Med Chem 66: 9363-9375 (2023)
Hepagene Therapeutics
SAR of L-ABBA analogs for GGT1 inhibitory activity and L-ABBA's effect on plasma cysteine and GSH species.
Bioorg Med Chem Lett 92: (2023)
State University of New York
Recent advances in Fragment-based strategies against tuberculosis.
NA
Univ. Lille
Discovery of 3-(1H-benzo[d]imidazole-2-yl)-1H-pyrazol-4 -amine derivatives as novel and potent syk inhibitors for the treatment of hematological malignancies.
NA
China Pharmaceutical University
Azaindole derivatives as potential kinase inhibitors and their SARs elucidation.
NA
Hunan University of Science and Technology
Design, synthesis and evaluation of novel 1-phenyl-pyrrolo[1,2-b]isoquinolin-3-one derivatives as antagonists for the glycine binding site of the NMDA receptor.
NA
Guizhou Medical University
Highly-tumor-targeted PAD4 inhibitors with PBA modification inhibit tumors in vivo by specifically inhibiting the PAD4-H3cit-NETs pathway in neutrophils.
NA
College of Pharmaceutical Sciences of Capital Medical University
The role of natural anti-parasitic guided development of synthetic drugs for leishmaniasis.
NA
Acharya & BM Reddy College of Pharmacy
Design, synthesis, and biological evaluation of a series of new anthraquinone derivatives as anti-ZIKV agents.
NA
Sun Yat-sen University
Development and pharmacological evaluation of a new chemical series of potent pan-ERR agonists, identification of SLU-PP-915.
NA
Saint Louis University School of Medicine
Discovery of novel hybrids of mTOR inhibitor and NO donor as potential anti-tumor therapeutics.
Bioorg Med Chem 91: (2023)
Anhui University of Chinese Medicine
Ligand-Directed Photodegradation of Interacting Proteins: Oxidative HER2/HER3 Heterodimer Degradation with a Lapatinib-Derived Photosensitizer.
J Med Chem 66: 10265-10272 (2023)
Shandong University
Discovery of Selective Dopamine Receptor Ligands Derived from (-)-Stepholidine via C-3 Alkoxylation and C-3/C-9 Dialkoxylation.
J Med Chem 66: 10060-10079 (2023)
City University of New York
Rational Design of RNA Demethylase FTO Inhibitors with Enhanced Antileukemia Drug-Like Properties.
J Med Chem 66: 9731-9752 (2023)
University of Chinese Academy of Sciences
Dual Piperidine-Based Histamine H
J Med Chem 66: 9658-9683 (2023)
Jagiellonian University Medical College
Reversal of subtype-selectivity and function by the introduction of a para-benzamidyl substituent to N-cyclopropylmethyl nornepenthone.
NA
Fudan University
N-aryltetrahydroisoquinoline derivatives as HA-CD44 interaction inhibitors: Design, synthesis, computational studies, and antitumor effect.
NA
University of Granada
Recent advances of targeting nicotinamide phosphoribosyltransferase (NAMPT) for cancer drug discovery.
NA
China Pharmaceutical University
Recent advances in the discovery of tropomyosin receptor kinases TRKs inhibitors: A mini review.
NA
Cairo University
Synthesis and evaluation of dihydrofuro[2,3-b]pyridine derivatives as potent IRAK4 inhibitors.
NA
Soochow University
Design, synthesis, and biological studies of novel sulfonamide derivatives as farnesoid X receptor agonists.
NA
Guangdong Pharmaceutical University
Design, synthesis, and biological evaluation of novel penindolone derivatives as potential inhibitors of hemagglutinin-mediated membrane fusion.
NA
Ocean University of China
Dimer Peptide Ligands of Vascular Endothelial Growth Factor: Optimizing Linker Length for High Affinity and Antiangiogenic Activity.
J Med Chem 66: 9753-9765 (2023)
University Paris Cite
Development of Biaryl-Containing Aldo-Keto Reductase 1C3 (AKR1C3) Inhibitors for Reversing AKR1C3-Mediated Drug Resistance in Cancer Treatment.
J Med Chem 66: 9537-9560 (2023)
China Pharmaceutical University
Development of novel PEX5-PEX14 protein-protein interaction (PPI) inhibitors based on an oxopiperazine template.
NA
Medical University of Warsaw
Discovery of YK-029A, a novel mutant EGFR inhibitor targeting both T790 M and exon 20 insertion mutations, as a treatment for NSCLC.
NA
Puhe Biopharma
Systematic Study of Heteroarene Stacking Using a Congeneric Set of Molecular Glues for Procaspase-6.
J Med Chem 66: 9784-9796 (2023)
University of California
Expanding Chemical Probe Space: Quality Criteria for Covalent and Degrader Probes.
J Med Chem 66: 9297-9312 (2023)
Merck Healthcare
The recent advance of Interleukin-1 receptor associated kinase 4 inhibitors for the treatment of inflammation and related diseases.
NA
Children's Hospital Affiliated to Zhengzhou University
Purine containing carbonucleoside phosphonate analogues as novel chemotype for Plasmodium falciparum Inhibition.
NA
CNRS-Univ Lyon 1
Discovery of benzofuran-2-carboxylic acid derivatives as lymphoid tyrosine phosphatase (LYP) inhibitors for cancer immunotherapy.
NA
Shandong University
Perspectives and new aspects of histone deacetylase inhibitors in the therapy of CNS diseases.
NA
Shanghai Institute of Pharmaceutical Industry Co., Ltd.
Identification of Brain-Penetrant ATP-Competitive mTOR Inhibitors for CNS Syndromes.
J Med Chem 66: 9095-9119 (2023)
Novartis Institutes for Biomedical Research
Modified Podophyllotoxin Phenoxyacetamide Phenylacetate Derivatives: Tubulin/AKT1 Dual-Targeting and Potential Anticancer Agents for Human NSCLC.
J Nat Prod 86: 1844-1854 (2023)
Changzhou University
Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRAS
J Med Chem 66: 9147-9160 (2023)
Astrazeneca
Discovery of tetrasubstituted thiophenes as Cisd2 activators: A potential novel therapeutic option in nonalcoholic fatty liver disease.
NA
National Health Research Institutes
Fluorine in anti-HIV drugs approved by FDA from 1981 to 2023.
NA
Shanghai University
Discovery of novel diarypyrimidine derivatives bearing six-membered non-aromatic heterocycles as potent HIV-1 NNRTIs with improved anti-resistance and drug-like profiles.
NA
Shandong University
SAR and lead optimization of (Z)-5-(4-hydroxy-3-methoxybenzylidene)-3-(2-morpholinoacetyl)thiazolidine-2,4-dione as a potential multi-target antidiabetic agent.
NA
COMSATS University Islamabad
Design, synthesis, activity and molecular dynamics studies of 1,3,4-thiadiazole derivatives as selective allosteric inhibitors of SHP2 for the treatment of cancer.
NA
Affiliated Hospital of Weifang Medical University
Development of submicromolar 17β-HSD10 inhibitors and their in vitro and in vivo evaluation.
NA
University of Hradec Kralove
Discovery of Acyl-Indole Derivatives as Pan-Serotype Dengue Virus NS4B Inhibitors.
J Med Chem 66: 8808-8821 (2023)
Janssen Research and Development
Discovery of NAFLD-Improving Agents by Promoting the Degradation of Keap1.
J Med Chem 66: 9184-9200 (2023)
China Pharmaceutical University
Alicyclic Ring Size Variation of 4-Phenyl-2-naphthoic Acid Derivatives as P2Y
J Med Chem 66: 9076-9094 (2023)
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of ARD-2051 as a Potent and Orally Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer.
J Med Chem 66: 8822-8843 (2023)
University of Michigan
Discovery of 1
J Med Chem 66: 8725-8744 (2023)
China Pharmaceutical University
Small molecule inhibitors of PCSK9. SAR investigations of head and amine groups.
Bioorg Med Chem Lett 92: (2023)
Pfizer
Design, synthesis and biological evaluation of nitric oxide-releasing 5-cyano-6-phenyl-2, 4-disubstituted pyrimidine derivatives.
Bioorg Med Chem Lett 92: (2023)
Zhengzhou University
Design, synthesis and mechanism studies of dual EZH2/BRD4 inhibitors for cancer therapy.
Bioorg Med Chem 91: (2023)
China Pharmaceutical University
Design, Synthesis, Molecular Docking, and Biological Evaluation of Novel Pimavanserin-Based Analogues as Potential Serotonin 5-HT
J Med Chem 66: 9057-9075 (2023)
The University of Jordan
Targeting the Estrogen Receptor for the Treatment of Breast Cancer: Recent Advances and Challenges.
J Med Chem 66: 8339-8381 (2023)
University of Michigan
Inhibitors for metallo-β-lactamases from the B1 and B3 subgroups provide an avenue to combat a major mechanism of antibiotic resistance.
Bioorg Med Chem Lett 92: (2023)
The University of Queensland
Discovery of potent NAMPT-Targeting PROTACs using FK866 as the warhead.
Bioorg Med Chem Lett 92: (2023)
Changzhou University
Research progress of STAT3-based dual inhibitors for cancer therapy.
Bioorg Med Chem 91: (2023)
Xinxiang University
Potent Dual Inhibitors of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 with a Suitable Pharmacokinetic Profile for
J Med Chem 66: 8975-8992 (2023)
Saarland University
Preferred Conformation-Guided Discovery of Potent and Orally Active HIF Prolyl Hydroxylase 2 Inhibitors for the Treatment of Anemia.
J Med Chem 66: 8545-8563 (2023)
China Pharmaceutical University
Targeting Arginine Methyltransferase PRMT5 for Cancer Therapy: Updated Progress and Novel Strategies.
J Med Chem 66: 8407-8427 (2023)
Sun Yat-Sen University
Synthesis and evaluation of Fmoc-amino esters and amides bearing a substrate like quaternary ammonium group as selective butyrylcholinesterase inhibitors.
Bioorg Med Chem Lett 92: (2023)
California State University
Design, synthesis, antiviral evaluation, and In silico studies of acrylamides targeting nsP2 from Chikungunya virus.
NA
Federal University of Alagoas
Scaffold hopping derived novel benzoxazepinone RIPK1 inhibitors as anti-necroptosis agents.
Bioorg Med Chem 91: (2023)
Ningxia Medical University
Medicinal chemistry approaches to target the MNK-eIF4E axis in cancer.
RSC Med Chem 14: 1060-1087 (2023)
Northwestern University
STING antagonists, synthesized
RSC Med Chem 14: 1101-1113 (2023)
Purdue University
Identification of macrocyclic peptides which activate bacterial cylindrical proteases.
RSC Med Chem 14: 1186-1191 (2023)
University of Cambridge
Small-molecule inhibitors of bacterial-producing metallo-β-lactamases: insights into their resistance mechanisms and biochemical analyses of their activities.
RSC Med Chem 14: 1012-1048 (2023)
University Sains Malaysia
Thiourea derivatives containing 4-arylthiazoles and d-glucose moiety: design, synthesis, antimicrobial activity evaluation, and molecular docking/dynamics simulations.
RSC Med Chem 14: 1114-1130 (2023)
Vietnam National University
Basic Nitrogen (BaN) Is a Key Property of Antimalarial Chemical Space.
J Med Chem 66: 8382-8406 (2023)
Birla Institute of Technology and Science Pilani
Discovery of novel hypoxia-activated, nitroimidazole constructed multi-target kinase inhibitors on the basis of AZD9291 for the treatment of human lung cancer.
Bioorg Med Chem 91: (2023)
Hangzhou City University
Recent research advances in ATX inhibitors: An overview of primary literature.
Bioorg Med Chem 90: (2023)
Weifang Medical University
Assessment of the structure-activity relationship and antileukemic activity of diacylpyramide compounds as human ClpP agonists.
NA
University of Chinese Academy of Sciences
Identification of small-molecule inhibitors of human MUS81-EME1/2 by FRET-based high-throughput screening.
Bioorg Med Chem 90: (2023)
Fuzhou University
Design, synthesis and evaluation the bioactivities of novel 1,3-dimethyl-6-amino-1H-indazole derivatives as anticancer agents.
Bioorg Med Chem 90: (2023)
Phenikaa University
Allosteric Inhibitors of Macrophage Migration Inhibitory Factor (MIF) Interfere with Apoptosis-Inducing Factor (AIF) Co-Localization to Prevent Parthanatos.
J Med Chem 66: 8767-8781 (2023)
University of Groningen
Discovery of 5-((1H-indazol-3-yl) methylene)-2-thioxoimidazolidin-4-one derivatives as a new class of AHR agonists with anti-psoriasis activity in a mouse model.
Bioorg Med Chem Lett 92: (2023)
Sichuan University
Design, synthesis and biological evaluation of 3-substituted-2-thioxothiazolidin-4-one (rhodanine) derivatives as antitubercular agents against Mycobacterium tuberculosis protein tyrosine phosphatase B.
NA
Peking Union Medical College and Chinese Academy of Medical Sciences
Novel spiroindoline quinazolinedione derivatives as anticancer agents and potential FLT3 kinase inhibitors.
Bioorg Med Chem 90: (2023)
Shiraz University of Medical Sciences
Discovery and Optimization of the First ATP Competitive Type-III c-MET Inhibitor.
J Med Chem 66: 8782-8807 (2023)
Astrazeneca
Structure-Activity Relationship Study of the High-Affinity Neuropeptide Y
J Med Chem 66: 8745-8766 (2023)
Leipzig University
Licochalcone A Derivatives as Selective Dipeptidyl Peptidase 4 Inhibitors with Anti-Inflammatory Effects.
J Nat Prod 86: 1824-1831 (2023)
Shanghai University of Traditional Chinese Medicine
Versatile anti-infective properties of pyrido- and dihydropyrido[2,3-d]pyrimidine-based compounds.
Bioorg Med Chem 90: (2023)
Qassim University
Design, synthesis, and analgesia evaluation of novel Transient Receptor Potential Vanilloid 1 (TRPV1) agonists modified from Cannabidiol (CBD).
Bioorg Med Chem 90: (2023)
Shanghai University of Traditional Chinese Medicine
Development and therapeutic potential of allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists for autoimmune diseases.
NA
Fudan University
Exploring N-myristoyltransferase as a promising drug target against parasitic neglected tropical diseases.
NA
State University of Paraiba
Discovery and Structural Optimization of Novel Quinolone Derivatives as Potent Irreversible Pan-Fibroblast Growth Factor Receptor Inhibitors for Treating Solid Tumors.
J Med Chem 66: 8858-8875 (2023)
Skyrun Pharma Co.
Design, Synthesis, and Pharmacological Characterization of a Potent Soluble Epoxide Hydrolase Inhibitor for the Treatment of Acute Pancreatitis.
J Med Chem 66: 9201-9222 (2023)
University of Salerno
Discovery of Pyxinol Amide Derivatives Bearing Amino Acid Residues as Nonsubstrate Allosteric Inhibitors of P-Glycoprotein-Mediated Multidrug Resistance.
J Med Chem 66: 8628-8642 (2023)
Yantai University
New aryl and acylsulfonamides as state-dependent inhibitors of Nav1.3 voltage-gated sodium channel.
NA
University of Ljubljana
Spiroindole-containing compounds bearing phosphonate group of potential Mpro-SARS-CoV-2 inhibitory properties.
NA
Augusta University
Discovery of N-(2-chloro-5-(3-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridin-5-yl)pyridin-3-yl)-4-fluorobenzenesulfonamide (FD274) as a highly potent PI3K/mTOR dual inhibitor for the treatment of acute myeloid leukemia.
NA
Fudan University
Development of diphenylmethylpiperazine hybrids of chloroquinoline and triazolopyrimidine using Petasis reaction as new cysteine proteases inhibitors for malaria therapeutics.
NA
Jamia Millia Islamia
Design and synthesis of 6-arylpyridine-tethered sulfonamides as novel selective inhibitors of carbonic anhydrase IX with promising antitumor features toward the human colorectal cancer.
NA
Kafrelsheikh University
Isolation and identification of the new baicalin target protein to develop flavonoid structure-based therapeutic agents.
Bioorg Med Chem 90: (2023)
Teikyo University
Development and Characterization of Potent Succinate Receptor Fluorescent Tracers.
J Med Chem 66: 8951-8974 (2023)
University of Copenhagen
Development of VER-50589 analogs as novel Hsp90 inhibitors.
Bioorg Med Chem Lett 91: (2023)
Qingdao University
Structure-activity relationship study of central pyridine-derived TYK2 JH2 inhibitors: Optimization of the PK profile through C4' and C6 variations.
Bioorg Med Chem Lett 91: (2023)
Bristol-Myers Squibb
Discovery of 4'-trifluoromethylchalcones as novel, potent and selective hCYP1B1 inhibitors without concomitant AhR activation.
NA
Shanghai University of Traditional Chinese Medicine
Eyes on Topical Ocular Disposition: The Considered Design of a Lead Janus Kinase (JAK) Inhibitor That Utilizes a Unique Azetidin-3-Amino Bridging Scaffold to Attenuate Off-Target Kinase Activity, While Driving Potency and Aqueous Solubility.
J Med Chem 66: 8929-8950 (2023)
Alcon Research
Design and Pharmacological Chaperone Effects of
J Med Chem 66: 9023-9039 (2023)
University of Toyama
Discovery of [1,2,3]Triazolo[4,5-
ACS Med Chem Lett 14: 746-756 (2023)
Sichuan University
Novel Concept for Super-Soft Topical Drugs: Deactivation by an Enzyme-Induced Switch into an Inactive Conformation.
ACS Med Chem Lett 14: 841-845 (2023)
Novartis Institutes For Biomedical Research
Novel Aryl Hydrocarbon Receptor Agonists for Treating Psoriasis.
ACS Med Chem Lett 14: 696-697 (2023)
Smith, Gambrell & Russell
Covalent
ACS Med Chem Lett 14: 777-787 (2023)
Johannes Gutenberg University Mainz
Novel IL4I1 Inhibitors for Treating Cancer.
ACS Med Chem Lett 14: 700-701 (2023)
Smith, Gambrell & Russell
Design, Synthesis, and Structure-Activity Relationships of Biaryl Anilines as Subtype-Selective PPAR-alpha Agonists.
ACS Med Chem Lett 14: 766-776 (2023)
University of Minnesota
DNA-Encoded Macrocyclic Peptide Libraries Enable the Discovery of a Neutral MDM2-p53 Inhibitor.
ACS Med Chem Lett 14: 820-826 (2023)
Unnatural Products
Novel 2,5-Diazabicyclo[4.2.0]octanes as GLP-1 Receptor Modulators for Treating Type 2 Diabetes.
ACS Med Chem Lett 14: 709-710 (2023)
Smith, Gambrell & Russell
-Aryl Indoles as a Novel Class of Potent Na
ACS Med Chem Lett 14: 788-793 (2023)
Daiichi Sankyo
Discovery of Selective and Potent KRAS
ACS Med Chem Lett 14: 689-691 (2023)
Usona Institute
Cyclopentathiophene Carboxamide Derivatives as PAFR Antagonists for Treating Ocular Diseases, Allergies, and Inflammation-Related Disorders.
ACS Med Chem Lett 14: 705-706 (2023)
Smith, Gambrell & Russell
Discovery of Novel Hydroxyimine-Tethered Benzenesulfonamides as Potential Human Carbonic Anhydrase IX/XII Inhibitors.
ACS Med Chem Lett 14: 810-819 (2023)
Jamia Millia Islamia
Discovery of Novel, Selective Prostaglandin EP4 Receptor Antagonists with Efficacy in Cancer Models.
ACS Med Chem Lett 14: 727-736 (2023)
Arromax Pharmatech Co.
Design and Synthesis of Pyrazole-Based Macrocyclic Kinase Inhibitors Targeting BMPR2.
ACS Med Chem Lett 14: 833-840 (2023)
Johann Wolfgang Goethe-University
Benziodarone and 6-hydroxybenziodarone are potent and selective inhibitors of transthyretin amyloidogenesis.
Bioorg Med Chem 90: (2023)
University of Toyama
Design and Synthesis of 4-Fluorophenyl-5-methylene-2(5
J Med Chem 66: 8441-8463 (2023)
Shandong University
Elucidation of novel TRAP1-Selective inhibitors that regulate mitochondrial processes.
NA
University of Notre Dame
Discovery and Structure-Based Design of Inhibitors of the WD Repeat-Containing Protein 5 (WDR5)-MYC Interaction.
J Med Chem 66: 8310-8323 (2023)
Novartis Institutes For Biomedical Research
Discovery of a Pan-Melanocortin Receptor Antagonist [Ac-DPhe(pI)-Arg-Nal(2')-Orn-NH
J Med Chem 66: 8103-8117 (2023)
University of Minnesota
Orally bioavailable styryl derivative of rohitukine-N-oxide inhibits CDK9/T1 and the growth of pancreatic cancer cells.
NA
CSIR-Indian Institute of Integrative Medicine
Advances in CD73 inhibitors for immunotherapy: Antibodies, synthetic small molecule compounds, and natural compounds.
NA
Chengdu University of Traditional Chinese Medicine
Structure-based virtual screening discovers potent and selective adenosine A
Eur J Med Chem 257: (2023)
Uppsala University
Pharmacological activity and mechanism of pyrazines.
NA
Gannan Medical University
Discovery of novel pyridinones as MGAT2 inhibitors for the treatment of metabolic disorders.
Bioorg Med Chem Lett 91: (2023)
Bristol Myers Squibb
Identification of 5-[5-cyano-1-(pyridin-2-ylmethyl)-1H-indole-3-carboxamido] thiazole-4-carboxylic acid as a promising dual inhibitor of urate transporter 1 and xanthine oxidase.
NA
Shenyang Pharmaceutical University
Evolution and Discovery of Matrine Derivatives as a New Class of Anti-Hepatic Fibrosis Agents Targeting Ewing Sarcoma Breakpoint Region 1 (EWSR1).
J Med Chem 66: 7969-7987 (2023)
Peking Union Medical College
Design and Synthesis of Inhibitors of the E3 Ligase SMAD Specific E3 Ubiquitin Protein Ligase 1 as a Treatment for Lung Remodeling in Pulmonary Arterial Hypertension.
J Med Chem 66: 8130-8139 (2023)
Novartis Institutes of Biomedical Research (NIBR)
Structure-Based Discovery of Inhibitors of the SARS-CoV-2 Nsp14 N7-Methyltransferase.
J Med Chem 66: 7785-7803 (2023)
University of California San Francisco
Structurally Diverse Triterpene-26-oic Acids as Potential Dual ACL and ACC1 Inhibitors from the Vulnerable Conifer
J Nat Prod 86: 1487-1499 (2023)
Fudan University
Discovery of a novel 1,3,4-oxadiazol-2-one-based NLRP3 inhibitor as a pharmacological agent to mitigate cardiac and metabolic complications in an experimental model of diet-induced metaflammation.
Eur J Med Chem 257: (2023)
University of Turin
Structure-based discovery of novel cruzain inhibitors with distinct trypanocidal activity profiles.
NA
Universidade Federal de Minas Gerais
Precise Conformational Control Yielding Highly Potent and Exceptionally Selective BRD4 Degraders with Strong Antitumor Activity.
J Med Chem 66: 8222-8237 (2023)
University of Michigan
Discovery of Novel 5,6-Dihydro-1,2,4-triazine Derivatives as Efficacious Glucagon-Like Peptide-1 Receptor Agonists.
J Med Chem 66: 7988-8010 (2023)
Shanghai Institute of Materia Medica
Research progress of VEGFR small molecule inhibitors in ocular neovascular diseases.
NA
Southwest Jiaotong University
The Role of Allylic Strain for Conformational Control in Medicinal Chemistry.
J Med Chem 66: 7730-7755 (2023)
Astrazeneca
TMPRSS2 Inhibitor Discovery Facilitated through an
ACS Med Chem Lett 14: 860-866 (2023)
University of Michigan
6-Substituted Triazolyl Benzoxaboroles as Selective Carbonic Anhydrase Inhibitors:
J Med Chem 66: 8118-8129 (2023)
University of Florence
Discovery and Design of Novel Cyclic Peptides as Specific Inhibitors Targeting CCN2 and Disrupting CCN2/EGFR Interaction for Kidney Fibrosis Treatment.
J Med Chem 66: 8251-8266 (2023)
Sun Yat-Sen University
Tuning the Metabolic Stability of Visual Cycle Modulators through Modification of an RPE65 Recognition Motif.
J Med Chem 66: 8140-8158 (2023)
University of California - Irvine
Discovery of the First Potent, Selective, and
J Med Chem 66: 8200-8221 (2023)
Shenyang Pharmaceutical University
Discovery of Exceptionally Potent, Selective, and Efficacious PROTAC Degraders of CBP and p300 Proteins.
J Med Chem 66: 8178-8199 (2023)
University of Michigan
The Zinc-Binding Group Effect: Lessons from Non-Hydroxamic Acid Vorinostat Analogs.
J Med Chem 66: 7698-7729 (2023)
Ghent University
Influence of N-arylsulfonamido d-valine N-substituents on the selectivity and potency of matrix metalloproteinase inhibitors.
Bioorg Med Chem 90: (2023)
University of Munster
Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors.
Bioorg Med Chem Lett 91: (2023)
Astrazeneca
Discovery of NXT-10796, an orally active, intestinally restricted EP4 agonist prodrug for the treatment of inflammatory bowel disease.
Bioorg Med Chem Lett 91: (2023)
Inception Sciences Canada
Design, synthesis and biological evaluation of phosphoroxy quinazoline derivatives as potential EGFR
Bioorg Med Chem 90: (2023)
Southeast University
Synthesis and bioevaluation of novel stilbene-based derivatives as tubulin/HDAC dual-target inhibitors with potent antitumor activities in vitro and in vivo.
NA
China Pharmaceutical University
Transient receptor potential ankyrin 1 (TRPA1) modulators: Recent update and future perspective.
NA
Sichuan University
Structure-Based Design and Characterization of the Highly Potent and Selective Covalent Inhibitors Targeting the Lysine Methyltransferases G9a/GLP.
J Med Chem 66: 8086-8102 (2023)
Sun Yat-Sen University
Discovery of Small-Molecule Degraders for Alpha-Synuclein Aggregates.
J Med Chem 66: 7926-7942 (2023)
Sun Yat-Sen University
Isolation of Anti-SARS-CoV-2 Natural Products Extracted from
J Nat Prod 86: 1428-1436 (2023)
National Taiwan University
Discovery of a high potent PIM kinase inhibitor for acute myeloid leukemia based on N-pyridinyl amide scaffold by optimizing the fragments toward to Lys67 and Asp128/Glu171.
NA
Fudan University
Characterization of a Potent and Orally Bioavailable Lys-Covalent Inhibitor of Apoptosis Protein (IAP) Antagonist.
J Med Chem 66: 8159-8169 (2023)
University of California
Targeting MET: Discovery of Small Molecule Inhibitors as Non-Small Cell Lung Cancer Therapy.
J Med Chem 66: 7670-7697 (2023)
Jinan University
Computational Design, Synthesis, and Biological Evaluation of Diimidazole Analogues Endowed with Dual PCSK9/HMG-CoAR-Inhibiting Activity.
J Med Chem 66: 7943-7958 (2023)
University of Milan
Discovery and development of small-molecule heparanase inhibitors.
Bioorg Med Chem 90: (2023)
University of Florida
Molecular-level strategic goals and repressors in Leishmaniasis - Integrated data to accelerate target-based heterocyclic scaffolds.
NA
Birla Institute of Technology and Science Pilani
Discovery of quinazolin-4-one-based non-covalent inhibitors targeting the severe acute respiratory syndrome coronavirus 2 main protease (SARS-CoV-2 M
Eur J Med Chem 257: (2023)
China Pharmaceutical University
Discovery of new tetrahydroisoquinolines as potent and selective LSD1 inhibitors for the treatment of MLL-rearranged leukemia.
NA
Zhejiang Ocean University
Aurones: A Promising Scaffold to Inhibit SARS-CoV-2 Replication.
J Nat Prod 86: 1536-1549 (2023)
Instituto Oswaldo Cruz
Design of Nurr1 Agonists
J Med Chem 66: 8170-8177 (2023)
Ludwig Maximilian University of Munich
Escaping from Flatland: Multiparameter Optimization Leads to the Discovery of Novel Tetrahydropyrido[4,3-
J Med Chem 66: 8643-8665 (2023)
Shandong University
Design, synthesis and biological evaluation of peptidomimetic benzothiazolyl ketones as 3CLpro inhibitors against SARS-CoV-2.
NA
Zhengzhou University
Advances in the development of Rho GTPase inhibitors.
Bioorg Med Chem 90: (2023)
Shanghai Jiao Tong University
CitA activity is modulated by cysteine oxidation and pyruvate binding.
RSC Med Chem 14: 921-933 (2023)
University of Nebraska
Identification and analysis of small molecule inhibitors of FosB from
RSC Med Chem 14: 947-956 (2023)
The University of Alabama
Insights into targeting SARS-CoV-2: design, synthesis,
RSC Med Chem 14: 899-920 (2023)
Egyptian Russian University
Identification of ARUK2002821 as an isoform-selective PI5P4Kα inhibitor.
RSC Med Chem 14: 934-946 (2023)
University of Cambridge
Improving binding entropy by higher ligand symmetry? - A case study with human matriptase.
RSC Med Chem 14: 969-982 (2023)
Johannes Gutenberg-University Staudingerweg
Investigating the interactions of flavonoids with human OATP2B1: inhibition assay, IC
RSC Med Chem 14: 890-898 (2023)
Soochow University
Synthesis and structure-activity relationship (SAR) studies of 1,2,3-triazole, amide, and ester-based benzothiazole derivatives as potential molecular probes for tau protein.
RSC Med Chem 14: 858-868 (2023)
University of Wollongong
Oxazolidinones as versatile scaffolds in medicinal chemistry.
RSC Med Chem 14: 823-847 (2023)
University College London
Synthesis and evaluation of piperazinotriazoles. Discovery of a potent and orally bioavailable neurokinin-3 receptor inhibitor.
NA
Binzhou Medical University
Structure-affinity relationships of stereoisomers of norbenzomorphan-derived σ2R/TMEM97 modulators.
NA
The University of Texas at Austin
The emerging role of mixed lineage kinase 3 (MLK3) and its potential as a target for neurodegenerative diseases therapies.
Eur J Med Chem 257: (2023)
Universidad Complutense De Madrid
The research progress of SARS-CoV-2 main protease inhibitors from 2020 to 2022.
Eur J Med Chem 257: (2023)
Shenyang Pharmaceutical University
HIV-1 protease inhibitors with a P1 phosphonate modification maintain potency against drug-resistant variants by increased interactions with flap residues.
NA
University of Massachusetts Chan Medical School
Discovery of the First Subnanomolar PPARα/δ Dual Agonist for the Treatment of Cholestatic Liver Diseases.
J Med Chem 66: 7331-7354 (2023)
China Pharmaceutical University
Design, synthesis and biological evaluation of novel indole-3-carboxylic acid derivatives with antihypertensive activity.
Bioorg Med Chem Lett 90: (2023)
Lomonosov Moscow State University
Novel drug-like fluorenyl derivatives as selective butyrylcholinesterase and β-amyloid inhibitors for the treatment of Alzheimer's disease.
Bioorg Med Chem 88: (2023)
Jagiellonian University Medical College
Discovery, structural optimization, and anti-tumor bioactivity evaluations of betulinic acid derivatives as a new type of RORγ antagonists.
NA
Nanjing University of Chinese Medicine
Challenges for the development of mutant isocitrate dehydrogenases 1 inhibitors to treat glioma.
NA
Nanjing University of Chinese Medicine
Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors.
J Med Chem 66: 7534-7552 (2023)
Biocon-Bristol Myers Squibb Research and Development Center
Investigation into the Mechanism of Action of the Tuberculosis Drug Candidate SQ109 and Its Metabolites and Analogues in Mycobacteria.
J Med Chem 66: 7553-7569 (2023)
University of Illinois At Urbana-Champaign
Novel Medicinal Chemistry Strategies Targeting CDK5 for Drug Discovery.
J Med Chem 66: 7140-7161 (2023)
Sichuan University
Design, synthesis and biological evaluation of 4-(4-aminophenoxy)picolinamide derivatives as potential antitumor agents.
NA
The First Affiliated Hospital of Wenzhou Medical University
Bench-to-bedside: Innovation of small molecule anti-SARS-CoV-2 drugs in China.
Eur J Med Chem 257: (2023)
Qufu Normal University
Carbohydrate Strengthens the Immunotherapeutic Effect of Small-Molecule PD-L1 Inhibitors.
J Med Chem 66: 7179-7204 (2023)
Zhejiang University
Design and Optimization of Novel Benzimidazole- and Imidazo[4,5-
J Med Chem 66: 7304-7330 (2023)
Eberhard Karls University of Tubingen
Synthesis and anti-inflammatory activity evaluation of NO-releasing furoxan/1,2,4-triazole hybrid derivatives.
NA
China Medical University
Sulfur-fluoride exchange (SuFEx)-enabled lead discovery of AChE inhibitors by fragment linking strategies.
NA
Anhui Medical University
A beginner's guide to current synthetic linker strategies towards VHL-recruiting PROTACs.
Bioorg Med Chem 88: (2023)
Newcastle University
Synthesis and evaluation of DAG-lactone derivatives with HIV-1 latency reversing activity.
Eur J Med Chem 256: (2023)
Tokyo Medical and Dental University (TMDU)
An Analysis of Successful Hit-to-Clinical Candidate Pairs.
J Med Chem 66: 7101-7139 (2023)
Jnana Therapeutics
Rational Design of Covalent Kinase Inhibitors by an Integrated Computational Workflow (Kin-Cov).
J Med Chem 66: 7405-7420 (2023)
Jinan University
Generation and structure-activity relationships of novel imidazo-thienopyridine based TLR7 agonists: application as payloads for immunostimulatory antibody drug-conjugates.
Bioorg Med Chem Lett 91: (2023)
Zymeworks
Development of isoselenazolium chlorides as selective pyruvate kinase isoform M2 inhibitors.
NA
Institute of Organic Synthesis
Discovery of highly potent and selective VEGFR2 kinase inhibitors for the treatment of rheumatoid arthritis.
NA
Anhui Medical University
Modifications of geldanamycin via CuAAC altering affinity to chaperone protein Hsp90 and cytotoxicity.
Eur J Med Chem 256: (2023)
Adam Mickiewicz University
Recent advances in the development of dual ALK/ROS1 inhibitors for non-small cell lung cancer therapy.
NA
Weifang Medical University
Recent advance of small-molecule drugs for clinical treatment of multiple myeloma.
NA
Jilin University
Structure-based discovery of IHMT-IDH1-053 as a potent irreversible IDH1 mutant selective inhibitor.
Eur J Med Chem 256: (2023)
Chinese Academy of Sciences
Optimization, and biological evaluation of 3-O-β-chacotriosyl betulinic acid amide derivatives as novel small-molecule Omicron.
Eur J Med Chem 256: (2023)
South China Agricultural University
Discovery of thiohydantoin based antagonists of androgen receptor with efficient degradation for the treatment of prostate cancer.
NA
China Pharmaceutical University
Current scenario of pyrazole hybrids with in vivo therapeutic potential against cancers.
NA
Huanghuai University
Design, synthesis, and evaluation of PD-1/PD-L1 small-molecule inhibitors bearing a rigid indane scaffold.
Eur J Med Chem 256: (2023)
China Pharmaceutical University
Discovery of a first-in-class Aurora A covalent inhibitor for the treatment of triple negative breast cancer.
Eur J Med Chem 256: (2023)
Sun Yat-Sen University
Discovery of Novel 1,3-Diphenylpyrazine Derivatives as Potent S-Phase Kinase-Associated Protein 2 (Skp2) Inhibitors for the Treatment of Cancer.
J Med Chem 66: 7221-7242 (2023)
Zhengzhou University
Structure-Based Development of Isoform-Selective Inhibitors of Casein Kinase 1ε vs Casein Kinase 1δ.
J Med Chem 66: 7162-7178 (2023)
The Scripps Research Institute
Discovery of a New-Generation S-Adenosylmethionine-Noncompetitive Covalent Inhibitor Targeting the Lysine Methyltransferase Enhancer of Zeste Homologue 2.
J Med Chem 66: 7629-7644 (2023)
Sun Yat-Sen University
Design, synthesis, and pharmacological evaluation of N-(3-carbamoyl-1H-pyrazol-4-yl)-1,3-oxazole-4-carboxamide derivatives as interleukin-1 receptor-associated kinase 4 inhibitors with reduced potential for cytochrome P450 1A2 induction.
Bioorg Med Chem 87: (2023)
Astellas Pharma
Small-molecule LRRK2 inhibitors for PD therapy: Current achievements and future perspectives.
Eur J Med Chem 256: (2023)
Sichuan University
Rational design and evaluation of 2-((pyrrol-2-yl)methylene)thiophen-4-ones as RNase L inhibitors.
Eur J Med Chem 256: (2023)
Max Planck Institute of Molecular Physiology
Novel AHR Agonists for Treating Psoriasis.
ACS Med Chem Lett 14: 543-544 (2023)
Smith, Gambrell & Russell
Rational Design of Highly Potent and Selective Covalent MAP2K7 Inhibitors.
ACS Med Chem Lett 14: 606-613 (2023)
Northwestern University
Addressing the Osimertinib Resistance Mutation EGFR-L858R/C797S with Reversible Aminopyrimidines.
ACS Med Chem Lett 14: 591-598 (2023)
Tu Dortmund University
Monoacylglycerol Lipase Modulators for Treating Autism Spectrum Disorders.
ACS Med Chem Lett 14: 545-546 (2023)
Smith, Gambrell & Russell
1,2,4-Triazine Derivatives as NLRP3 Inhibitors for Treating Diseases.
ACS Med Chem Lett 14: 547-548 (2023)
Smith, Gambrell & Russell
Novel Serine-Arginine Protein Kinase Inhibitors for Treating Cancer.
ACS Med Chem Lett 14: 551-552 (2023)
Smith, Gambrell & Russell
PROTAC: Harnessing Targeted Chimeras for Selective BCL-2 Degradation in Cancer Treatment.
ACS Med Chem Lett 14: 541-542 (2023)
Usona Institute
Synthesis of Veliparib Prodrugs and Determination of Drug-Release-Dependent PARP-1 Inhibition.
ACS Med Chem Lett 14: 652-657 (2023)
University of Pittsburgh
Cytosolic Enzymes Generate Cannabinoid Metabolites 7-Carboxycannabidiol and 11-Nor-9-carboxytetrahydrocannabinol.
ACS Med Chem Lett 14: 614-620 (2023)
University of North Carolina at Chapel Hill
Inhibition of Thiamine Diphosphate-Dependent Enzymes by Triazole-Based Thiamine Analogues.
ACS Med Chem Lett 14: 621-628 (2023)
University of Cambridge
Selective Wee1 Inhibitors Led to Antitumor Activity
ACS Med Chem Lett 14: 566-576 (2023)
Emd Serono
Novel Thienopyrrole Compounds for Treating Autoimmune Diseases and Inflammatory Conditions.
ACS Med Chem Lett 14: 549-550 (2023)
Smith, Gambrell & Russell
Discovery of a Novel Series of Potent SHP2 Allosteric Inhibitors.
ACS Med Chem Lett 14: 645-651 (2023)
IRBM
Methyl and Fluorine Effects in Novel Orally Bioavailable Keap1-Nrf2 PPI Inhibitor.
ACS Med Chem Lett 14: 658-665 (2023)
Japan Tobacco
Inside PD-1/PD-L1,2 with their inhibitors.
Eur J Med Chem 256: (2023)
Nantes University
Design, synthesis, and anticancer evaluation of arylurea derivatives as potent and selective type II irreversible covalent FGFR4 inhibitors.
Bioorg Med Chem 87: (2023)
China Pharmaceutical University
Forrestiacids E-K: Further [4 + 2]-Type Triterpene-Diterpene Hybrids as Potential ACL Inhibitors from the Vulnerable Conifer
J Nat Prod 86: 1251-1260 (2023)
Taizhou University
Discovery of Novel Bruton's Tyrosine Kinase PROTACs with Enhanced Selectivity and Cellular Efficacy.
J Med Chem 66: 7454-7474 (2023)
Stony Brook University
Structure-guided optimization of adenosine mimetics as selective and potent inhibitors of coronavirus nsp14 N7-methyltransferases.
Eur J Med Chem 256: (2023)
University of Montpellier
-Guided Rational Drug Design and Synthesis of Novel 4-(Thiophen-2-yl)butanamides as Potent and Selective TRPV1 Agonists.
J Med Chem 66: 6994-7015 (2023)
Magna Gracia University
Discovery of an Anti-TNF-α 9-mer Peptide from a T7 Phage Display Library for the Treatment of Inflammatory Bowel Disease.
J Med Chem 66: 6981-6993 (2023)
Tongji University
Synthesis and Development of Highly Selective Pyrrolo[2,3-
J Med Chem 66: 6959-6980 (2023)
Norwegian University of Science and Technology (NTNU)
Evaluating the druggability of TrmD, a potential antibacterial target, through design and microbiological profiling of a series of potent TrmD inhibitors.
Bioorg Med Chem Lett 90: (2023)
Infex Therapeutics
Optimization and evaluation of pyridinyl vinyl sulfones as Nrf2 activator for the antioxidant and anti-inflammatory effects.
Eur J Med Chem 256: (2023)
Korea Institute of Science and Technology (KIST)
Design, synthesis and biological evaluation of covalent peptidomimetic 3CL protease inhibitors containing nitrile moiety.
Bioorg Med Chem 87: (2023)
An Hui University of Traditional Chinese Medicine
Fragment-Based Approaches to Identify RNA Binders.
J Med Chem 66: 6523-6541 (2023)
The Scripps Research Institute
Newly Synthesized 3-Indolyl Furanoid Inhibits Matrix Metalloproteinase-9 Activity and Prevents Nonsteroidal Anti-inflammatory Drug-Induced Gastric Ulceration.
J Med Chem 66: 8917-8928 (2023)
TBA
Discovery of (
J Med Chem 66: 7016-7037 (2023)
Shanghai Institute of Materia Medica
Discovery of novel bicyclic[3.3.0]proline peptidyl α-ketoamides as potent 3CL-protease inhibitors for SARS-CoV-2.
Bioorg Med Chem Lett 90: (2023)
Sun Yat-Sen University
Identification of (-)-Epigallocateshin gallate derivatives promoting innate immune activation via 2',3'-cyclic GMP-AMP-stimulator of interferon genes pathway.
Bioorg Med Chem Lett 90: (2023)
Korea Institute of Science and Technology
The lipidation and glycosylation enabling bioactivity enhancement and structural change of antibacterial peptide G3.
Bioorg Med Chem Lett 90: (2023)
Fujian Normal University
NSD3: Advances in cancer therapeutic potential and inhibitors research.
Eur J Med Chem 256: (2023)
Peking University
Synthesis of new multitarget-directed ligands containing thienopyrimidine nucleus for inhibition of 15-lipoxygenase, cyclooxygenases, and pro-inflammatory cytokines.
Eur J Med Chem 256: (2023)
Zagazig University
A cyanine-based NIR fluorescent Vemurafenib analog to probe BRAF
Eur J Med Chem 256: (2023)
University of Pisa
Bioisosteric replacement based on 1,2,4-oxadiazoles in the discovery of 1H-indazole-bearing neuroprotective MAO B inhibitors.
Eur J Med Chem 255: (2023)
University of Bari Aldo Moro
Current advances of small molecule E3 ligands for proteolysis-targeting chimeras design.
Eur J Med Chem 256: (2023)
East China Normal University
Targeting VPS34 in autophagy: An update on pharmacological small-molecule compounds.
Eur J Med Chem 256: (2023)
Southwest Jiaotong University
Discovery of pyrimidine-5-carboxamide derivatives as novel salt-inducible kinases (SIKs) inhibitors for inflammatory bowel disease (IBD) treatment.
Eur J Med Chem 256: (2023)
Sichuan University
Oxazole-4-carboxamide/butylated hydroxytoluene hybrids with GSK-3β inhibitory and neuroprotective activities against Alzheimer's disease.
Eur J Med Chem 256: (2023)
China Pharmaceutical University
Aporphines: A privileged scaffold in CNS drug discovery.
Eur J Med Chem 256: (2023)
Soochow University
Design, synthesis, and biological activity of dual monoamine oxidase A and heat shock protein 90 inhibitors, N-Methylpropargylamine-conjugated 4-isopropylresorcinol for glioblastoma.
Eur J Med Chem 256: (2023)
University of Southern California
Discovery, Synthesis, and In Vitro Characterization of 2,3 Derivatives of 4,5,6,7-Tetrahydro-Benzothiophene as Potent Modulators of Retinoic Acid Receptor-Related Orphan Receptor γt.
J Med Chem 66: 7355-7373 (2023)
Mcgill University
Discovery of novel triazine derivatives as potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists.
Eur J Med Chem 256: (2023)
Fudan University
Discovery of pyrido[4,3-d]pyrimidinone derivatives as novel Wee1 inhibitors.
Bioorg Med Chem 87: (2023)
Zhejiang University
Rational design of 4-((6-phenoxypyrimidin-4-yl)amino)-N-(4-(piperazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide (LT-540-717) as orally bioavailable FLT3 inhibitor.
Eur J Med Chem 256: (2023)
Henan University of Chinese Medicine
Selective Estrogen receptor degraders (SERDs) for the treatment of breast cancer: An overview.
Eur J Med Chem 256: (2023)
Central University of Punjab
Design, synthesis and pharmacological evaluation of 2,3-dihydrobenzofuran IRAK4 inhibitors for the treatment of diffuse large B-cell lymphoma.
Eur J Med Chem 256: (2023)
China Pharmaceutical University
Discovery of 2,5-diaminopyrimidine derivatives as the first series of selective monomeric degraders of B-lymphoid tyrosine kinase.
Eur J Med Chem 256: (2023)
Peking University
Discovery of C-5 Pyrazole-Substituted Pyrrolopyridine Derivatives as Potent and Selective Inhibitors for Janus Kinase 1.
J Med Chem 66: 6725-6742 (2023)
University of South China
Small-Molecule Modulators Targeting Toll-like Receptors for Potential Anticancer Therapeutics.
J Med Chem 66: 6437-6462 (2023)
West China Hospital
Design and Characterization of Squaramic Acid-Based Prostate-Specific Membrane Antigen Inhibitors for Prostate Cancer.
J Med Chem 66: 6889-6904 (2023)
Beijing Normal University
Discovery of a Novel Class of PROTACs as Potent and Selective Estrogen Receptor α Degraders to Overcome Endocrine-Resistant Breast Cancer
J Med Chem 66: 6631-6651 (2023)
Zhongnan Hospital of Wuhan University
Perspectives on the current antiviral developments towards RNA-dependent RNA polymerase (RdRp) and methyltransferase (MTase) domains of dengue virus non-structural protein 5 (DENV-NS5).
Eur J Med Chem 256: (2023)
Csir-Indian Institute of Chemical Technology (CSIR-IICT)
Quinazoline-2-Carboxamides as Selective PET Radiotracers for Matrix Metalloproteinase-13 Imaging in Atherosclerosis.
J Med Chem 66: 6682-6696 (2023)
University of Ottawa
Design, synthesis and biological evaluation of novel indole-piperazine derivatives as antibacterial agents.
Bioorg Med Chem Lett 89: (2023)
Northwest A&F University
Synthesis-accessibility-oriented design of c-Jun N-terminal kinase 1 inhibitor.
Eur J Med Chem 256: (2023)
East China University of Science and Technology
Recent advances in EZH2-based dual inhibitors in the treatment of cancers.
Eur J Med Chem 256: (2023)
Xinxiang University
First-in-Class Selective Inhibitors of the Lysine Acetyltransferase KAT8.
J Med Chem 66: 6591-6616 (2023)
Sapienza University of Rome
Exploration of imatinib and nilotinib-derived templates as the P2-Ligand for HIV-1 protease inhibitors: Design, synthesis, protein X-ray structural studies, and biological evaluation.
Eur J Med Chem 255: (2023)
Purdue University
Design and synthesis of a novel class of PDE4 inhibitors with antioxidant properties as bifunctional agents for the potential treatment of COPD.
Eur J Med Chem 256: (2023)
China Pharmaceutical University
Clinically approved small-molecule drugs for the treatment of rheumatoid arthritis.
Eur J Med Chem 256: (2023)
Jilin University
A Molecular Toolbox of Positron Emission Tomography Tracers for General Anesthesia Mechanism Research.
J Med Chem 66: 6463-6497 (2023)
Xiamen University
X-ray Crystal Structure-Guided Discovery of Novel Indole Analogues as Colchicine-Binding Site Tubulin Inhibitors with Immune-Potentiating and Antitumor Effects against Melanoma.
J Med Chem 66: 6697-6714 (2023)
Southern Medical University
A highly selective purine-based inhibitor of CSF1R potently inhibits osteoclast differentiation.
Eur J Med Chem 255: (2023)
Norwegian University of Science and Technology (Ntnu
Discovery of Potent and Wild-Type-Sparing Fourth-Generation EGFR Inhibitors for Treatment of Osimertinib-Resistance NSCLC.
J Med Chem 66: 6849-6868 (2023)
China Pharmaceutical University
Development of a fluorescence screening assay for binding partners of the iron-sulfur mitochondrial protein mitoNEET.
Bioorg Med Chem Lett 89: (2023)
West Virginia University
Design, synthesis, and biological evaluation of acyl sulfonamide derivatives with spiro cycles as Na
Bioorg Med Chem 86: (2023)
Fudan University
Design, Synthesis, Biological Evaluation, and Crystallographic Study of Novel Purine Nucleoside Phosphorylase Inhibitors.
J Med Chem 66: 6652-6681 (2023)
The Czech Academy of Sciences
Design, Synthesis, and Evaluation of (
J Med Chem 66: 6905-6921 (2023)
Jinan University
Small Molecules Targeting DNA Polymerase Theta (POLθ) as Promising Synthetic Lethal Agents for Precision Cancer Therapy.
J Med Chem 66: 6498-6522 (2023)
University of Perugia
Ψ and χ Angle Constrains at the C-Terminus Trp Position of the Melanotropin Tetrapeptide Ac-His-d-Phe-Arg-Trp-NH
J Med Chem 66: 6715-6724 (2023)
The University of Arizona
Discovery of Thieno[3,2-d]pyrimidine derivatives as potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) kinase.
Eur J Med Chem 255: (2023)
China Pharmaceutical University
-Phenyl-1-(phenylsulfonyl)-1
J Med Chem 66: 6193-6217 (2023)
Collaborations Pharmaceuticals
Design, Synthesis, and Bioevaluation of Novel MyD88 Inhibitor c17 against Acute Lung Injury Derived from the Virtual Screen.
J Med Chem 66: 6938-6958 (2023)
Wenzhou Medical University
Transformation of a Dopamine D
J Med Chem 66: 6274-6287 (2023)
Shanghaitech University
Dual-Acting Small Molecules: Subtype-Selective Cannabinoid Receptor 2 Agonist/Butyrylcholinesterase Inhibitor Hybrids Show Neuroprotection in an Alzheimer's Disease Mouse Model.
J Med Chem 66: 6414-6435 (2023)
Julius Maximilian University Wuerzburg
Development of a Potent Nurr1 Agonist Tool for In Vivo Applications.
J Med Chem 66: 6391-6402 (2023)
Ludwig Maximilian University of Munich
Synthesis of novel ciprofloxacin-avibactam conjugates for the development of second-generation non-β-lactam-β-lactamase inhibitors.
Bioorg Med Chem Lett 88: (2023)
CSIR-Institute of Himalayan Bioresource Technology
Discovery of imidazo[1,2-b]pyridazine macrocyclic derivatives as novel ALK inhibitors capable of combating multiple resistant mutants.
Bioorg Med Chem Lett 89: (2023)
Shanghai Institute of Pharmaceutical Industry Co.
Discovery of 4-oxo-4,5-dihydropyrazolo[1,5-a]quinoxaline-7-carboxamide derivatives as PI3Kα inhibitors via virtual screening and docking-based structure optimization.
Bioorg Med Chem 86: (2023)
Zhejiang University
Synthesis of the Purported Structure of Glyphaeaside C and Proposed Revisions to the Structures of the Glyphaeaside Alkaloids.
J Nat Prod 86: 1261-1273 (2023)
University of Wollongong
Discovery of new 5-substituted-indole-2-carboxamides as dual epidermal growth factor receptor (EGFR)/cyclin dependent kinase-2 (CDK2) inhibitors with potent antiproliferative action.
RSC Med Chem 14: 734-744 (2023)
Jouf University Al-Qurayyat
Development of thiazole-appended novel hydrazones as a new class of α-amylase inhibitors with anticancer assets: an
RSC Med Chem 14: 757-781 (2023)
Ccs Haryana Agricultural University
Ribosome-targeting antibiotics and resistance
RSC Med Chem 14: 624-643 (2023)
Emory University
Computational design of a cyclic peptide that inhibits the CTLA4 immune checkpoint.
RSC Med Chem 14: 658-670 (2023)
Kansas State University
Semisynthetic blasticidin S ester derivatives show enhanced antibiotic activity.
RSC Med Chem 14: 782-789 (2023)
Virginia Tech
Comprehensive coverage on anti-mycobacterial endeavour reported during 2022.
Eur J Med Chem 255: (2023)
L. M. College of Pharmacy
Design, synthesis, and biological evaluation of novel HIV-1 protease inhibitors containing pyrrolidine-derived P2 ligands to combat drug-resistant variant.
Eur J Med Chem 255: (2023)
Chinese Academy of Medical Science and Peking Union Medical College
Conformationally locked sugar derivatives and analogues as potential neuraminidase inhibitors.
Eur J Med Chem 255: (2023)
Jawaharlal Nehru University
Discovery of a Novel Series of Potent, Selective, Orally Available, and Brain-Penetrable C1s Inhibitors for Modulation of the Complement Pathway.
J Med Chem 66: 6354-6371 (2023)
Takeda Pharmaceutical
Phthalazinone-based lactams and cyclic ureas as ROCK2 selective inhibitors.
Bioorg Med Chem Lett 88: (2023)
Bristol Myers Squibb
Discovery of novel BTK PROTACs with improved metabolic stability via linker rigidification strategy.
Eur J Med Chem 255: (2023)
Fudan University
Optimization of 3-aminotetrahydrothiophene 1,1-dioxides with improved potency and efficacy as non-electrophilic antioxidant response element (ARE) activators.
Bioorg Med Chem Lett 89: (2023)
Pusan National University
Design, synthesis, and biological evaluation of novel HDAC inhibitors with a 3-(benzazol-2-yl)quinoxaline framework.
Bioorg Med Chem Lett 88: (2023)
Southeast University
Halo Library, a Tool for Rapid Identification of Ligand Binding Sites on Proteins Using Crystallographic Fragment Screening.
J Med Chem 66: 6013-6024 (2023)
Rutgers University
Filling a nick in NIK: Extending the half-life of a NIK inhibitor through structure-based drug design.
Bioorg Med Chem Lett 89: (2023)
Genentech
Design, synthesis, and anti-inflammatory activity characterization of novel brain-permeable HDAC6 inhibitors.
Eur J Med Chem 254: (2023)
Chinese Academy of Sciences
Deciphering the multifunctional role of dual leucine zipper kinase (DLK) and its therapeutic potential in disease.
Eur J Med Chem 255: (2023)
Southwest Jiaotong University
Identification of Binding Sites in the Nucleotide-Binding Domain of P-Glycoprotein for a Potent and Nontoxic Modulator, the Amine-Containing Monomeric Flavonoid
J Med Chem 66: 6160-6183 (2023)
The Hong Kong Polytechnic University
Stapled Peptides as Direct Inhibitors of Nrf2-sMAF Transcription Factors.
J Med Chem 66: 6184-6192 (2023)
Purdue University
Identification of a novel spirocyclic Nek2 inhibitor using high throughput virtual screening.
Bioorg Med Chem Lett 88: (2023)
Queens College of the City University of New York
Neurotensin(8-13) analogs as dual NTS1 and NTS2 receptor ligands with enhanced effects on a mouse model of Parkinson's disease.
Eur J Med Chem 254: (2023)
University of Bonn
Shifting the selectivity of pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors towards the salt-inducible kinase (SIK) subfamily.
Eur J Med Chem 254: (2023)
Johann Wolfgang Goethe University
Identification of small molecule inhibitors against MMP-14 via High-Throughput screening.
Bioorg Med Chem 85: (2023)
University of Illinois at Chicago
Structure-Activity Relationships Reveal Beneficial Selectivity Profiles of Inhibitors Targeting Acetylcholinesterase of Disease-Transmitting Mosquitoes.
J Med Chem 66: 6333-6353 (2023)
Umea University
Carbamate JNK3 Inhibitors Show Promise as Effective Treatments for Alzheimer's Disease: In Vivo Studies on Mouse Models.
J Med Chem 66: 6372-6390 (2023)
Hanyang University
Enzymatic transformation of esculetin as a potent class of α-glucosidase inhibitors.
Bioorg Med Chem Lett 88: (2023)
Korea Atomic Energy Research Institute (KAERI)
Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells.
Eur J Med Chem 254: (2023)
Peking University
Synthesis and evaluation of sulfonamide derivatives targeting EGFR
Bioorg Med Chem 85: (2023)
Shenyang Pharmaceutical University
Discovery of novel, potent, and orally bioavailable HDACs inhibitors with LSD1 inhibitory activity for the treatment of solid tumors.
Eur J Med Chem 254: (2023)
Xinxiang Medical University
Discovery of selective Na
Eur J Med Chem 254: (2023)
Shanghai Institute of Materia Medica
Selective degradation of cellular BRD3 and BRD4-L promoted by PROTAC molecules in six cancer cell lines.
Eur J Med Chem 254: (2023)
Shanghai Institute of Materia Medica
Dihydrotrichodimerol Purified from the Marine Fungus
J Nat Prod 86: 1189-1201 (2023)
Xiamen University
Structure-guided design of direct-acting antivirals that exploit the gem-dimethyl effect and potently inhibit 3CL proteases of severe acute respiratory syndrome Coronavirus-2 (SARS-CoV-2) and middle east respiratory syndrome coronavirus (MERS-CoV).
Eur J Med Chem 254: (2023)
Wichita State University
Design, synthesis and bioactivity evaluations of 8-substituted-quinoline-2-carboxamide derivatives as novel histone deacetylase (HDAC) inhibitors.
Bioorg Med Chem 85: (2023)
Shandong University
Discovery of the First-in-Class Intestinal Restricted FXR and FABP1 Dual Modulator ZLY28 for the Treatment of Nonalcoholic Fatty Liver Disease.
J Med Chem 66: 6082-6104 (2023)
Guangdong Pharmaceutical University
Targeting the "Undruggable" Driver Protein, KRAS
ACS Med Chem Lett 14: 365-366 (2023)
Usona Institute
Discovery and Optimization of a Novel Macrocyclic Amidinourea Series Active as Acidic Mammalian Chitinase Inhibitors.
ACS Med Chem Lett 14: 417-424 (2023)
University of Siena
The Identification of GPR52 Agonist HTL0041178, a Potential Therapy for Schizophrenia and Related Psychiatric Disorders.
ACS Med Chem Lett 14: 499-505 (2023)
Sosei Heptares
Development and Characterization of Fluorescent Probes for the G Protein-Coupled Receptor 35.
ACS Med Chem Lett 14: 411-416 (2023)
Dalian Institute of Chemical Physics
Rimonabant-Based Compounds Bearing Hydrophobic Amino Acid Derivatives as Cannabinoid Receptor Subtype 1 Ligands.
ACS Med Chem Lett 14: 479-486 (2023)
Hun Biological Research Centre, Szeged
Prenylated Chrysin Derivatives as Partial PPARγ Agonists with Adiponectin Secretion-Inducing Activity.
ACS Med Chem Lett 14: 425-431 (2023)
Seoul National University
Discovery of Futibatinib: The First Covalent FGFR Kinase Inhibitor in Clinical Use.
ACS Med Chem Lett 14: 396-404 (2023)
Taiho Pharmaceutical
Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2.
ACS Med Chem Lett 14: 432-441 (2023)
University of North Carolina at Chapel Hill
Cyclic Peptidic Furin Inhibitors Developed by Combinatorial Chemistry.
ACS Med Chem Lett 14: 458-465 (2023)
University of Gdansk
Accelerating Drug Discovery: Synthesis of Complex Chemotypes via Multicomponent Reactions.
ACS Med Chem Lett 14: 376-385 (2023)
Atavistik Bio
Discovery of Potent Deuterated Compounds as Potential KRAS
ACS Med Chem Lett 14: 362-364 (2023)
Usona Institute
Anagrelide: A Clinically Effective cAMP Phosphodiesterase 3A Inhibitor with Molecular Glue Properties.
ACS Med Chem Lett 14: 350-361 (2023)
The Baruch S. Blumberg Institute
Discovery of novel papain-like protease inhibitors for potential treatment of COVID-19.
Eur J Med Chem 254: (2023)
University of Sharjah
Structure-based discovery of potent USP28 inhibitors derived from Vismodegib.
Eur J Med Chem 254: (2023)
Anhui University of Chinese Medicine
Bifunctional degraders of cyclin dependent kinase 9 (CDK9): Probing the relationship between linker length, properties, and selective protein degradation.
Eur J Med Chem 254: (2023)
The Ohio State University
Rapid Elaboration of Fragments into Leads Applied to Bromodomain-3 Extra-Terminal Domain.
J Med Chem 66: 5859-5872 (2023)
Monash University (Parkville Campus)
Design, synthesis and biological evaluation of pyrrolopyrimidine derivatives as novel and selective positive modulator of the small conductance Ca
Eur J Med Chem 254: (2023)
Hebei Medical University
Discovery of 7H-Pyrrolo[2,3-d]pyrimidine Derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors.
Eur J Med Chem 254: (2023)
Shanghai Institute of Materia Medica
Synthesis and biological evaluation of novel pteridin-7(8H)-one derivatives as potent CDK2 inhibitors.
Bioorg Med Chem Lett 88: (2023)
Jiangnan University
Discovery of novel sulfonamide chromone-oxime derivatives as potent indoleamine 2,3-dioxygenase 1 inhibitors.
Eur J Med Chem 254: (2023)
Guilin Medical University
Discovery of bipyridine amide derivatives targeting pRXRα-PLK1 interaction for anticancer therapy.
Eur J Med Chem 254: (2023)
Xiamen University
Structure-Based Discovery of a New Selectivity-Enabling Motif for the FK506-Binding Protein 51.
J Med Chem 66: 5965-5980 (2023)
Technical University Darmstadt
Exploration of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Bispecific Inhibitors Based on the Moiety of Fedratinib for Treatment of Both Hematologic Malignancies and Solid Cancers.
J Med Chem 66: 5753-5773 (2023)
China Pharmaceutical University
Synthesis and analysis of novel catecholic ligands as inhibitors of catechol-O-methyltransferase.
Bioorg Med Chem Lett 88: (2023)
University of California at San Francisco
3-Arylidene-2-oxindoles as GSK3β inhibitors and anti-thrombotic agents.
Bioorg Med Chem Lett 87: (2023)
Volgograd State Medical University
Synthesis and biological evaluation of biaryl alkyl ethers as inhibitors of IDO1.
Bioorg Med Chem Lett 88: (2023)
Bristol Myers Squibb
Hydrazinecarbonyl-thiazol-2-acetamides with pronounced apoptotic behavior: synthesis, in vitro/in vivo anti-proliferative activity and molecular modeling simulations.
Bioorg Med Chem Lett 87: (2023)
Mansoura University
Design, synthesis and biological evaluation of novel thiosemicarbazones as cruzipain inhibitors.
Eur J Med Chem 254: (2023)
Universidad De Buenos Aires
Studies on diketopiperazine and dipeptide analogs as opioid receptor ligands.
Eur J Med Chem 254: (2023)
Texas Tech University Health Sciences Center
Dual function of protein phosphatase 5 (PPP5C): An emerging therapeutic target for drug discovery.
Eur J Med Chem 254: (2023)
China Pharmaceutical University
Multicomponent Petasis reaction for the identification of pyrazine based multi-target directed anti-Alzheimer's agents: In-silico design, synthesis, and characterization.
Eur J Med Chem 254: (2023)
Jamia Millia Islamia
New and promising type of leukotriene B4 (LTB4) antagonists based on the 1,4-benzodioxine structure.
Eur J Med Chem 254: (2023)
Sultan Moulay Slimane University
Discovery of quinazolin-4(3H)-one derivatives as novel AChE inhibitors with anti-inflammatory activities.
Eur J Med Chem 254: (2023)
Ocean University of China
Broad-spectrum coronavirus 3C-like protease peptidomimetic inhibitors effectively block SARS-CoV-2 replication in cells: Design, synthesis, biological evaluation, and X-ray structure determination.
Eur J Med Chem 253: (2023)
University of Naples Federico Ii
Design, Synthesis, and Antitumor Activity of Potent and Selective EGFR L858R/T790M Inhibitors and Identification of a Combination Therapy to Overcome Acquired Resistance in Models of Non-small-cell Lung Cancer.
J Med Chem 66: 5719-5752 (2023)
Sichuan University
Discovery of BRD4-HDAC Dual Inhibitors with Improved Fungal Selectivity and Potent Synergistic Antifungal Activity against Fluconazole-Resistant
J Med Chem 66: 5950-5964 (2023)
East China University of Science & Technology
Optimization of potent, selective and orally bioavailable biphenyl scaffold as FABP4 inhibitors for anti-inflammation.
Eur J Med Chem 253: (2023)
Fudan University
Structure-guided identification of novel dual-targeting estrogen receptor α degraders with aromatase inhibitory activity for the treatment of endocrine-resistant breast cancer.
Eur J Med Chem 253: (2023)
Zhongnan Hospital of Wuhan University
Advances of bioorthogonal coupling reactions in drug development.
Eur J Med Chem 253: (2023)
China Pharmaceutical University
Design, synthesis and in vitro/in vivo anticancer activity of tranylcypromine-based triazolopyrimidine analogs as novel LSD1 inhibitors.
Eur J Med Chem 253: (2023)
Henan University of Chinese Medicine
Discovery of pyrazolo[3,4-b]pyridine derivatives as novel and potent Mps1 inhibitors for the treatment of cancer.
Eur J Med Chem 253: (2023)
Nanjing University of Chinese Medicine
Factor XIa Inhibitors in Anticoagulation Therapy: Recent Advances and Perspectives.
J Med Chem 66: 5332-5363 (2023)
Hefei University of Technology
Inhibition of the hERG potassium ion channel by different non-nucleoside human cytomegalovirus polymerase antiviral inhibitor series and the exploration of variations on a pyrroloquinoline core to reduce cardiotoxicity potential.
Bioorg Med Chem 85: (2023)
University of Alberta
Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions.
J Med Chem 66: 5524-5535 (2023)
Dana-Farber Cancer Institute
Siderophores: Chemical tools for precise antibiotic delivery.
Bioorg Med Chem Lett 87: (2023)
Universidade De Santiago De Compostela
Identification of a Noxo1 inhibitor by addition of a polyethylene glycol chain.
Bioorg Med Chem 85: (2023)
University of Cincinnati
Synthesis and anti-Alzheimer potential of novel α-amino phosphonate derivatives and probing their molecular interaction mechanism with acetylcholinesterase.
Eur J Med Chem 253: (2023)
Yogi Vemana University
Bacterial GTPases as druggable targets to tackle antimicrobial resistance.
Bioorg Med Chem Lett 87: (2023)
Indian Institute of Science Education and Research Bhopal
Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities.
Bioorg Med Chem 85: (2023)
Bristol Myers Squibb
Design, synthesis and biological evaluation of novel indolin-2-one derivatives as potent second-generation TRKs inhibitors.
Eur J Med Chem 253: (2023)
Shenyang Pharmaceutical University
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Inhibitors of CDK8 for the Treatment of Cancer.
J Med Chem 66: 5439-5452 (2023)
Insilico Medicine Shanghai
Discovery of FXR/PPARγ dual partial agonist.
Bioorg Med Chem 85: (2023)
Hiroshima International University
Discovery of novel arylpiperazine-based DA/5-HT modulators as potential antipsychotic agents - Design, synthesis, structural studies and pharmacological profiling.
Eur J Med Chem 252: (2023)
Medical University of Lublin
Development of Orally Bioavailable Amidobenzimidazole Analogues Targeting Stimulator of Interferon Gene (STING) Receptor.
J Med Chem 66: 5584-5610 (2023)
China Pharmaceutical University
Identification of a Selective SCoR2 Inhibitor That Protects Against Acute Kidney Injury.
J Med Chem 66: 5657-5668 (2023)
Case Western Reserve University School of Medicine
Acetyl-Click Screening Platform Identifies Small-Molecule Inhibitors of Histone Acetyltransferase 1 (HAT1).
J Med Chem 66: 5774-5801 (2023)
Wayne State University
Small molecule LpxC inhibitors against gram-negative bacteria: Advances and future perspectives.
Eur J Med Chem 253: (2023)
Sichuan University
Discovery of a potent and selective allosteric inhibitor targeting the SHP2 tunnel site for RTK-driven cancer treatment.
Eur J Med Chem 253: (2023)
Hangzhou Medical College
Atropo/Tropo Flexibility: A Tool for Design and Synthesis of Self-Adaptable Inhibitors of Carbonic Anhydrases and Their Antiproliferative Effect.
J Med Chem 66: 5703-5718 (2023)
Latvian Institute of Organic Synthesis
Discovery of Dual Lysine Methyltransferase G9a and EZH2 Inhibitors with In Vivo Efficacy against Malignant Rhabdoid Tumor.
J Med Chem 66: 5685-5702 (2023)
Shenyang Pharmaceutical University
An ATG4B inhibitor blocks autophagy and sensitizes Sorafenib inhibition activities in HCC tumor cells.
Bioorg Med Chem 84: (2023)
Yantai University
Discovery of Novel Sesquiterpene Lactone Derivatives as Potent PKM2 Activators for the Treatment of Ulcerative Colitis.
J Med Chem 66: 5500-5523 (2023)
Nanjing University of Chinese Medicine
Lysine-Specific Demethylase 1 Promises to Be a Novel Target in Cancer Drug Resistance: Therapeutic Implications.
J Med Chem 66: 4275-4293 (2023)
Zhengzhou University
"Magic Chloro": Profound Effects of the Chlorine Atom in Drug Discovery.
J Med Chem 66: 5305-5331 (2023)
The Scripps Research Institute
Discovery of the First Raptor (Regulatory-Associated Protein of mTOR) Inhibitor as a New Type of Antiadipogenic Agent.
J Med Chem 66: 5839-5858 (2023)
Sun Yat-Sen University
Advances in Epilepsy: Mechanisms, Clinical Trials, and Drug Therapies.
J Med Chem 66: 4434-4467 (2023)
Sichuan University
Design, synthesis and biological evaluation of quinazoline SOS1 inhibitors.
Bioorg Med Chem Lett 88: (2023)
Jiangnan University
Design, synthesis and bioactivity evaluation of a series of quinazolinone derivatives as potent PI3Kγ antagonist.
Bioorg Med Chem 84: (2023)
Southern Medical University
Palbociclib and Michael-acceptor hybrid compounds as CDK4/6 covalent inhibitors: Improved potency, broad anticancer spectrum and overcoming drug resistance.
Bioorg Med Chem 84: (2023)
Southeast University
Novel Benzo Five-Membered Heterocycle Derivatives as P-Glycoprotein Inhibitors: Design, Synthesis, Molecular Docking, and Anti-Multidrug Resistance Activity.
J Med Chem 66: 5550-5566 (2023)
Zhejiang University
2-Aminobenzoxazole Derivatives as Potent Inhibitors of the Sphingosine-1-Phosphate Transporter Spinster Homolog 2 (Spns2).
J Med Chem 66: 5873-5891 (2023)
Virginia Tech
Novel thienocycloalkylpyridazinones as useful scaffolds for acetylcholinesterase inhibition and serotonin 5-HT
Bioorg Med Chem 84: (2023)
University of Sassari
Machine learning- and structure-based discovery of a novel chemotype as FXR agonists for potential treatment of nonalcoholic fatty liver disease.
Eur J Med Chem 252: (2023)
Chinese Academy of Medical Sciences&Peking Union Medical College
Modulation of ERK5 Activity as a Therapeutic Anti-Cancer Strategy.
J Med Chem 66: 4491-4502 (2023)
Newcastle University Centre for Cancer
Design, synthesis and evaluation of novel monoamine oxidase B (MAO-B) inhibitors with improved pharmacokinetic properties for Parkinson's disease.
Eur J Med Chem 252: (2023)
Hec Pharm Group
Discovery of SYD5115, a novel orally active small molecule TSH-R antagonist.
Bioorg Med Chem 84: (2023)
Byondis
Designing Smaller, Synthetic, Functional Mimetics of Sulfated Glycosaminoglycans as Allosteric Modulators of Coagulation Factors.
J Med Chem 66: 4503-4531 (2023)
Virginia Commonwealth University
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