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Design, synthesis and biological evaluation of dual Topo II/HDAC inhibitors bearing pyrimido[5,4-b]indole and pyrazolo[3,4-d]pyrimidine motifs.
Eur J Med Chem 252: (2023)
Hebei University
Falcipains: Biochemistry, target validation and structure-activity relationship studies of inhibitors as antimalarials.
Eur J Med Chem 252: (2023)
University of Petroleum and Energy Studies
Highly selective butyrylcholinesterase inhibitors related to Amaryllidaceae alkaloids - Design, synthesis, and biological evaluation.
Eur J Med Chem 252: (2023)
Charles University
Targeting glutaminase 1 (GLS1) by small molecules for anticancer therapeutics.
Eur J Med Chem 252: (2023)
Sichuan University
Fragment Hopping-Based Design of Novel Biphenyl-DAPY Derivatives as Potent Non-Nucleoside Reverse Transcriptase Inhibitors Featuring Significantly Improved Anti-Resistance Efficacy.
J Med Chem 66: 4755-4767 (2023)
Fudan University
Structure-activity relationship analysis of activity-based probes targeting HTRA family of serine proteases.
Bioorg Med Chem Lett 87: (2023)
Gwangju Institute of Science and Technology
Synthesis and biological evaluation of DIDS analogues as efficient inhibitors of RAD51 involved in homologous recombination.
Bioorg Med Chem Lett 87: (2023)
Nantes Universite
An overview of compound properties, multiparameter optimization, and computational drug design methods for PARP-1 inhibitor drugs.
Eur J Med Chem 252: (2023)
Niper Guwahati
Structure-based discovery of novel α-aminoketone derivatives as dual p53-MDM2/MDMX inhibitors for the treatment of cancer.
Eur J Med Chem 252: (2023)
Nanjing University of Chinese Medicine
Optimization of the C2 substituents on the 1,4-bis(arylsulfonamido)naphthalene-N,N'-diacetic acid scaffold for better inhibition of Keap1-Nrf2 protein-protein interaction.
Eur J Med Chem 252: (2023)
The State University of New Jersey
Discovery of a Potent and Selective CCR8 Small Molecular Antagonist IPG7236 for the Treatment of Cancer.
J Med Chem 66: 4548-4564 (2023)
TBA
Discovery and Binding Mechanism of Pyrazoloisoquinoline-Based Novel β-Arrestin Inverse Agonists of the Kappa-Opioid Receptor.
J Med Chem 66: 5154-5170 (2023)
Gwangju Institute of Science and Technology (GIST)
Development of Son of Sevenless Homologue 1 (SOS1) Modulators To Treat Cancers by Regulating RAS Signaling.
J Med Chem 66: 4324-4341 (2023)
China Pharmaceutical University
Design and Pharmacological Characterization of α
J Med Chem 66: 5021-5040 (2023)
University of Bologna
Novel Aryl Sulfonamide Derivatives as NLRP3 Inflammasome Inhibitors for the Potential Treatment of Cancer.
J Med Chem 66: 5223-5241 (2023)
University of Ferrara
Perspective for Discovery of Small Molecule IL-6 Inhibitors through Study of Structure-Activity Relationships and Molecular Docking.
J Med Chem 66: 4417-4433 (2023)
Dongguk University
Design and synthesis of naturally-inspired SARS-CoV-2 inhibitors.
RSC Med Chem 14: 507-519 (2023)
Institut Pasteur
Structural rationalization of GSPT1 and IKZF1 degradation by thalidomide molecular glue derivatives.
RSC Med Chem 14: 501-506 (2023)
Dana-Farber Cancer Institute
Identification of a new class of proteasome inhibitors based on a naphthyl-azotricyclic-urea-phenyl scaffold.
RSC Med Chem 14: 573-582 (2023)
Middlesex University
Quinazolinone-1,2,3-triazole-acetamide conjugates as potent α-glucosidase inhibitors: synthesis, enzyme inhibition, kinetic analysis, and molecular docking study.
RSC Med Chem 14: 520-533 (2023)
Tehran University of Medical Sciences Tehran Iran
Structure-Activity Relationships of Truncated 1'-Homologated Carbaadenosine Derivatives as New PPARγ/δ Ligands: A Study on Sugar Puckering Affecting Binding to PPARs.
J Med Chem 66: 4961-4978 (2023)
Seoul National University
Synthesis and SAR of a novel Kir6.2/SUR1 channel opener scaffold identified by HTS.
Bioorg Med Chem Lett 87: (2023)
Vanderbilt University
Small molecule-based fluorescent probes for the detection of α-Synuclein aggregation states.
Bioorg Med Chem Lett 86: (2023)
Csir-Indian Institute of Chemical Technology (CSIR-IICT)
Bis-chalcones: A review of synthetic methodologies and anti-inflammatory effects.
Eur J Med Chem 252: (2023)
University of Porto
Repurposing 1,2,4-oxadiazoles as SARS-CoV-2 PLpro inhibitors and investigation of their possible viral entry blockade potential.
Eur J Med Chem 252: (2023)
Alexandria University
The discovery of cyclic γ-AApeptides as the promising ligands targeting EP2.
Bioorg Med Chem Lett 87: (2023)
University of South Florida
Potential RNA-dependent RNA polymerase (RdRp) inhibitors as prospective drug candidates for SARS-CoV-2.
Eur J Med Chem 252: (2023)
National Research Centre
Isosteviol derivatives as protein tyrosine Phosphatase-1B inhibitors: Synthesis, biological evaluation and molecular docking.
Bioorg Med Chem 83: (2023)
Shanghai Ocean University
Design and Structural Optimization of Methionine Adenosyltransferase 2A (MAT2A) Inhibitors with High In Vivo Potency and Oral Bioavailability.
J Med Chem 66: 4849-4867 (2023)
Guizhou University
Discovery of Potent and Highly Selective Interleukin-2-Inducible T-Cell Kinase Degraders with
J Med Chem 66: 4979-4998 (2023)
Peking University
Recent advances in the development of methyltransferase (MTase) inhibitors against (re)emerging arboviruses diseases dengue and Zika.
Eur J Med Chem 252: (2023)
Instituto Politecnico Nacional
Differentiating Inhibition Selectivity and Binding Affinity of Isocitrate Dehydrogenase 1 Variant Inhibitors.
J Med Chem 66: 5279-5288 (2023)
University of Oxford
Development and Therapeutic Implications of Tyrosine Kinase 2 Inhibitors.
J Med Chem 66: 4378-4416 (2023)
China Pharmaceutical University
Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2-
J Med Chem 66: 4231-4252 (2023)
Biocon-Bristol Myers Squibb Research and Development Center
Discovery of Nanomolar DCAF1 Small Molecule Ligands.
J Med Chem 66: 5041-5060 (2023)
University of Toronto
Conformationally Restricted σ
J Med Chem 66: 4999-5020 (2023)
Westf£Lische Wilhelms-Universit£T M£Nster
Discovery of novel N-benzylarylamide-dithiocarbamate based derivatives as dual inhibitors of tubulin polymerization and LSD1 that inhibit gastric cancers.
Eur J Med Chem 252: (2023)
Zhengzhou University
Design, synthesis, and biological evaluation of diaryl heterocyclic derivatives targeting tubulin polymerization with potent anticancer activities.
Eur J Med Chem 252: (2023)
Guangdong Academy of Sciences
Design and Synthesis of Functionally Active 5-Amino-6-Aryl Pyrrolopyrimidine Inhibitors of Hematopoietic Progenitor Kinase 1.
J Med Chem 66: 4888-4909 (2023)
Pfizer
Application and Study of ROCK Inhibitors in Pulmonary Fibrosis: Recent Developments and Future Perspectives.
J Med Chem 66: 4342-4360 (2023)
Sichuan University
Discovery of a PDZ Domain Inhibitor Targeting the Syndecan/Syntenin Protein-Protein Interaction: A Semi-Automated "Hit Identification-to-Optimization" Approach.
J Med Chem 66: 4633-4658 (2023)
Aix-Marseille University
Development of sulfonium tethered peptides conjugated with HDAC inhibitor to improve selective toxicity for cancer cells.
Bioorg Med Chem 83: (2023)
Tongji Medical College Huazhong University of Science and Technology
Designed switch from covalent to non-covalent inhibitors of carboxylesterase Notum activity.
Eur J Med Chem 251: (2023)
University College London
Designed multiple ligands for the treatment of type 2 diabetes mellitus and its complications: Discovery of (5-arylidene-4-oxo-2-thioxothiazolidin-3-yl)alkanoic acids active as novel dual-targeted PTP1B/AKR1B1 inhibitors.
Eur J Med Chem 252: (2023)
University of Messina
Design and Synthesis of Triazole-Containing HDAC Inhibitors That Induce Antitumor Effects and Immune Response.
J Med Chem 66: 4802-4826 (2023)
Xuzhou Medical University
Discovery of orally effective and safe GPR40 agonists by incorporating a chiral, rigid and polar sulfoxide into β-position to the carboxylic acid.
Eur J Med Chem 251: (2023)
Soochow University
BAY-6096: A Potent, Selective, and Highly Water-Soluble Adrenergic α
J Med Chem 66: 4659-4670 (2023)
Bayer
Discovery of a novel 1H-pyrazole- [3,4-b] pyridine-based lysine demethylase 5B inhibitor with potential anti-prostate cancer activity that perturbs the phosphoinositide 3-kinase/AKT pathway.
Eur J Med Chem 251: (2023)
Zhengzhou University
Discovery of N-substituted oseltamivir derivatives as novel neuraminidase inhibitors with improved drug resistance profiles and favorable drug-like properties.
Eur J Med Chem 252: (2023)
Shandong University
Discovery of 3-phenyl-1,2,4-oxadiazole derivatives as a new class of SARS-CoV-2 main protease inhibitors.
Bioorg Med Chem Lett 86: (2023)
Sichuan University
Discovery of a brain-sparing GIRK1/4 inhibitor for pharmacological cardioversion of atrial fibrillation.
Bioorg Med Chem Lett 85: (2023)
Novartis Institutes For Biomedical Research
Optimization of triazolo[4,5-d]pyrimidines towards human CC chemokine receptor 7 (CCR7) antagonists.
Eur J Med Chem 251: (2023)
Ku Leuven
Optically activated MEK1/2 inhibitors (Opti-MEKi) as potential antimelanoma agents.
Eur J Med Chem 251: (2023)
Peking University
Introducing Conformational Restraints on 25CN-NBOH: A Selective 5-HT
ACS Med Chem Lett 14: 319-325 (2023)
University of Copenhagen
Trust Your Gut: Strategies and Tactics for Intestinally Restricted Drugs.
ACS Med Chem Lett 14: 233-243 (2023)
Genentech
Controlling Ibrutinib's Conformations about Its Heterobiaryl Axis to Increase BTK Selectivity.
ACS Med Chem Lett 14: 305-311 (2023)
San Diego State University
Accelerated Discovery of Macrocyclic CDK2 Inhibitor QR-6401 by Generative Models and Structure-Based Drug Design.
ACS Med Chem Lett 14: 297-304 (2023)
Tencent Ai Lab
Contemporary Progress and Opportunities in RNA-Targeted Drug Discovery.
ACS Med Chem Lett 14: 251-259 (2023)
University of Michigan
Ligand Screening System for the RXRα Heterodimer Using the Fluorescence RXR Agonist CU-6PMN.
ACS Med Chem Lett 14: 291-296 (2023)
University of Shizuoka
Discovery of Orally Bioavailable FGFR2/FGFR3 Dual Inhibitors via Structure-Guided Scaffold Repurposing Approach.
ACS Med Chem Lett 14: 312-318 (2023)
Incyte
Antitumor effect of 3-(quinolin-2-ylmethylene)-4,6-dimethyl-5-hydroxy-7-azaoxindole down-regulating the Gas6-Axl axis.
Eur J Med Chem 251: (2023)
Yeungnam University
Discovery of novel benzamide derivatives bearing benzamidophenyl and phenylacetamidophenyl scaffolds as potential antitumor agents via targeting PARP-1.
Eur J Med Chem 251: (2023)
Sun Yat-Sen University
Development of the "hidden" multi-target-directed ligands by AChE/BuChE for the treatment of Alzheimer's disease.
Eur J Med Chem 251: (2023)
Guizhou Medical University
Probing Ligand Binding Sites on Large Proteins by Nuclear Magnetic Resonance Spectroscopy of Genetically Encoded Non-Canonical Amino Acids.
J Med Chem 66: 5289-5304 (2023)
Australian National University
Development of Fluorescent 4-[4-(3
J Med Chem 66: 3798-3817 (2023)
University of Bari Aldo Moro
Design, synthesis and biological evaluation of Nucleosidic CD99 inhibitors that selectively reduce Ewing sarcoma viability.
Eur J Med Chem 251: (2023)
Georgetown University
Therapeutic potential of targeting kynurenine pathway in neurodegenerative diseases.
Eur J Med Chem 251: (2023)
Shaoxing University
Structure-Activity Relationships of Ligand Binding to Oxysterol-Binding Protein (OSBP) and OSBP-Related Protein 4.
J Med Chem 66: 3866-3875 (2023)
University of Oklahoma
Discovery of acridine-based LSD1 inhibitors as immune activators targeting LSD1 in gastric cancer.
Eur J Med Chem 251: (2023)
Zhengzhou University
Discovery of BGB-8035, a Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase for B-Cell Malignancies and Autoimmune Diseases.
J Med Chem 66: 4025-4044 (2023)
Beigene (Beijing) Co.
Targeting Receptor-Interacting Protein Kinase 1 by Novel Benzothiazole Derivatives: Treatment of Acute Lung Injury through the Necroptosis Pathway.
J Med Chem 66: 5261-5278 (2023)
Ningxia Medical University
Design, synthesis and biological evaluation of novel N-(methyl-d
Bioorg Med Chem Lett 86: (2023)
Nanjing University of Science and Technology
Discovery and anti-tumor activity of 4-(benzylamino)-6-(3,5-dimethylisoxazol-4-yl)quinolin-2(1H)-one (CG13250), a potent, selective and orally bioavailable BET bromodomain inhibitor.
Bioorg Med Chem Lett 86: (2023)
University of Maryland
Optimization of carbazole carboxamide RORγt agonists: Challenges in improving the metabolic stability and maintaining the agonistic activity.
Eur J Med Chem 251: (2023)
Fudan University
Discovery of 3,5-diaryl-1H-pyrazol-based ureas as potent RET inhibitors.
Eur J Med Chem 251: (2023)
Jinan University
RSK inhibitors as potential anticancer agents: Discovery, optimization, and challenges.
Eur J Med Chem 251: (2023)
Sichuan University
From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors.
Eur J Med Chem 251: (2023)
University of Belgrade
Discovery of a Potent, Cooperative, and Selective SOS1 PROTAC ZZ151 with In Vivo Antitumor Efficacy in KRAS-Mutant Cancers.
J Med Chem 66: 4197-4214 (2023)
Shanghai Institute of Materia Medica
Discovery of Linvencorvir (RG7907), a Hepatitis B Virus Core Protein Allosteric Modulator, for the Treatment of Chronic HBV Infection.
J Med Chem 66: 4253-4270 (2023)
China Innovation Center of Roche
Oxazolidinone: A promising scaffold for the development of antibacterial drugs.
NA
Children's Hospital Affiliated to Zhengzhou University
Recent updates on 1,2,3-triazole-containing hybrids with in vivo therapeutic potential against cancers: A mini-review.
Eur J Med Chem 251: (2023)
Wuhan University of Science and Technology
N-sulfonyl peptide-hybrids as a new class of dengue virus protease inhibitors.
Eur J Med Chem 251: (2023)
Heidelberg University
Korupensamine A, but not its atropisomer, korupensamine B, inhibits SARS-CoV-2 in vitro by targeting its main protease (M
Eur J Med Chem 251: (2023)
Nahda University
From lead to clinic: A review of the structural design of P2X7R antagonists.
Eur J Med Chem 251: (2023)
Sichuan University
Recent advances of mitochondrial complex I inhibitors for cancer therapy: Current status and future perspectives.
Eur J Med Chem 251: (2023)
Sichuan University
Synthesis and biological evaluation of coumarin derivatives as selective CYP2A6 inhibitors.
Bioorg Med Chem Lett 86: (2023)
Health Sciences University of Hokkaido
Discovery of a novel oral type Ⅰ CDK8 inhibitor against acute myeloid leukemia.
Eur J Med Chem 251: (2023)
Anhui Medical University
Design, synthesis, and biological evaluation of novel dihydropteridone derivatives possessing oxadiazoles moiety as potent inhibitors of PLK1.
Eur J Med Chem 251: (2023)
Shenyang Pharmaceutical University
Simple monocyclic pyrimidine analogs as microtubule targeting agents binding to the colchicine site.
Bioorg Med Chem 82: (2023)
Duquesne University
Silmitasertib (CX-4945), a Clinically Used CK2-Kinase Inhibitor with Additional Effects on GSK3β and DYRK1A Kinases: A Structural Perspective.
J Med Chem 66: 4009-4024 (2023)
Jagiellonian University
Discovery of Clinical Candidate ACT-777991, a Potent CXCR3 Antagonist for Antigen-Driven and Inflammatory Pathologies.
J Med Chem 66: 4179-4196 (2023)
Idorsia Pharmaceuticals
Discovery of Novel Substrate-Competitive Lysine Methyltransferase G9a Inhibitors as Anticancer Agents.
J Med Chem 66: 4059-4085 (2023)
Kyorin Pharmaceutical
Discovery of novel tranylcypromine-based derivatives as LSD1 inhibitors for gastric cancer treatment.
Eur J Med Chem 251: (2023)
Zhengzhou University
Synthesis and Anti-Inflammatory Activity of the Natural Cyclooxygenase-2 Inhibitor Axinelline A and Its Analogues.
J Nat Prod 86: 958-965 (2023)
Zhejiang University
Characterization of Serrulatane Diterpenoids in
J Nat Prod 86: 694-709 (2023)
University of Copenhagen
Design, synthesis and characterisation of a novel type II B-RAF paradox breaker inhibitor.
Eur J Med Chem 250: (2023)
University of Orleans
New Dual Inhibitors of Bacterial Topoisomerases with Broad-Spectrum Antibacterial Activity and In Vivo Efficacy against Vancomycin-Intermediate
J Med Chem 66: 3968-3994 (2023)
University of Ljubljana
Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases.
J Med Chem 66: 4106-4130 (2023)
Perha Pharmaceuticals
Design, synthesis, and biological testing of biphenylmethyloxazole inhibitors targeting HIV-1 reverse transcriptase.
Bioorg Med Chem Lett 84: (2023)
Yale University
Discovery of 2-aminoquinolone acid derivatives as potent inhibitors of SARS-CoV-2.
Bioorg Med Chem Lett 85: (2023)
Seoul National University
Identification and in silicon binding study of a novel NR2B selective NMDAR antagonist.
Bioorg Med Chem Lett 85: (2023)
Shenyang Pharmaceutical University
The activity and mechanism of vidofludimus as a potent enzyme inhibitor against NDM-1-positive E. coli.
Eur J Med Chem 250: (2023)
Northeast Agricultural University
Drug repurposing of propafenone to discover novel anti-tumor agents by impairing homologous recombination to delay DNA damage recovery of rare disease conjunctival melanoma.
Eur J Med Chem 250: (2023)
East China University of Science and Technology
Dipeptide-Derived Alkynes as Potent and Selective Irreversible Inhibitors of Cysteine Cathepsins.
J Med Chem 66: 3818-3851 (2023)
Helmholtz-Zentrum Dresden-Rossendorf
Recent advances in nuclear receptor-binding SET domain 2 (NSD2) inhibitors: An update and perspectives.
Eur J Med Chem 250: (2023)
China Pharmaceutical University
Anti-Aβ42 Aggregative Polyketides from the Antarctic Psychrophilic Fungus
J Nat Prod 86: 882-890 (2023)
Ocean University of China
Synthesis and biological evaluation of N-(3-fluorobenzyl)-4-(1-(methyl-d
Bioorg Med Chem Lett 85: (2023)
Sungkyunkwan University
Discovery of novel 5-(2-hydroxyphenyl)-2-phthalide-3(3H)-pyrazolones as balanced multifunctional agents against Alzheimer's disease.
NA
Sichuan University
Antitarget, Anti-SARS-CoV-2 Leads, Drugs, and the Drug Discovery-Genetics Alliance Perspective.
J Med Chem 66: 3664-3702 (2023)
University of Siena
Phenothiazine-Based LSD1 Inhibitor Promotes T-Cell Killing Response of Gastric Cancer Cells.
J Med Chem 66: 3896-3916 (2023)
Zhengzhou University
Structural Dynamics-Driven Discovery of Anticancer and Antimetastatic Effects of Diltiazem and Glibenclamide Targeting Urokinase Receptor.
J Med Chem 66: 5415-5426 (2023)
Fuzhou University
Discovery of PIM-1 kinase inhibitors based on the 2,5-disubstituted 1,3,4-oxadiazole scaffold against prostate cancer: Design, synthesis, in vitro and in vivo cytotoxicity investigation.
Eur J Med Chem 250: (2023)
Le Mans University
Discovery of 2-Aminopyrimidines as Potent Agonists for the Bitter Taste Receptor TAS2R14.
J Med Chem 66: 3499-3521 (2023)
Friedrich-Alexander-Universitat Erlangen-Nurnberg
Novel irreversible peptidic inhibitors of transglutaminase 2.
RSC Med Chem 14: 378-385 (2023)
University of Ottawa
Inactivation of myostatin by photooxygenation using functionalized d-peptides.
RSC Med Chem 14: 386-392 (2023)
Tokyo University
X-ray structure of human aldo-keto reductase 1C3 in complex with a bile acid fused tetrazole inhibitor: experimental validation, molecular docking and structural analysis.
RSC Med Chem 14: 341-355 (2023)
University of Novi
The war on hTG2: warhead optimization in small molecule human tissue transglutaminase inhibitors.
RSC Med Chem 14: 277-298 (2023)
University of Ottawa
Synthesis and properties of the kojic acid dimer and its potential for the treatment of Alzheimer's disease.
RSC Med Chem 14: 268-276 (2023)
Fujian Medical University
Pyridine based dual binding site aromatase (CYP19A1) inhibitors.
RSC Med Chem 14: 356-366 (2023)
Cardiff University
QSAR, structure-based pharmacophore modelling and biological evaluation of novel platelet ADP receptor (P2Y
RSC Med Chem 14: 239-246 (2023)
Al-Ahliyya Amman University
Design, synthesis, biological evaluation of urea substituted 1,2,5-oxadiazole-3-carboximidamides as novel indoleamine 2,3-dioxygenase-1 (IDO1) inhibitors.
Eur J Med Chem 250: (2023)
China Pharmaceutical University
The discovery of 12β-methyl-17-epi-18-nor-bile acids as potent and selective TGR5 agonists.
Eur J Med Chem 250: (2023)
Victoria University of Wellington
Discovery and structure-activity relationship study of 2-piperazinyl-benzothiazole derivatives as potent and selective PPARδ agonists.
Bioorg Med Chem 82: (2023)
Shionogi
Development, validation, and evaluation of a deep learning model to screen cyclin-dependent kinase 12 inhibitors in cancers.
Eur J Med Chem 250: (2023)
Peking Union Medical College
Modified Akuamma Alkaloids with Increased Potency at the Mu-opioid Receptor.
J Med Chem 66: 3312-3326 (2023)
University of Illinois Chicago
Development of a Covalent Inhibitor of c-Jun N-Terminal Protein Kinase (JNK) 2/3 with Selectivity over JNK1.
J Med Chem 66: 3356-3371 (2023)
Stanford University
Metabolism-Guided Selective Androgen Receptor Antagonists: Design, Synthesis, and Biological Evaluation for Activity against Enzalutamide-Resistant Prostate Cancer.
J Med Chem 66: 3372-3392 (2023)
University of Tennessee Health Science Center
Novel Pyrido[2',1':2,3]imidazo[4,5-
J Med Chem 66: 3411-3430 (2023)
Indian Association for the Cultivation of Science
Discovery of non-boronic acid Arginase 1 inhibitors through virtual screening and biophysical methods.
Bioorg Med Chem Lett 84: (2023)
Merck
E3 Ligases Meet Their Match: Fragment-Based Approaches to Discover New E3 Ligands and to Unravel E3 Biology.
J Med Chem 66: 3173-3194 (2023)
Astrazeneca
Discovery of 4-(1,2,4-Oxadiazol-5-yl)azepan-2-one Derivatives as a New Class of Cannabinoid Type 2 Receptor Agonists for the Treatment of Inflammatory Pain.
J Med Chem 66: 3460-3483 (2023)
Sichuan University
Optimization of 2,3-Dihydroquinazolinone-3-carboxamides as Antimalarials Targeting PfATP4.
J Med Chem 66: 3540-3565 (2023)
The Walter and Eliza Hall Institute of Medical Research
Targeting the Epidermal Growth Factor Receptor with Molecular Degraders: State-of-the-Art and Future Opportunities.
J Med Chem 66: 3135-3172 (2023)
Central University of Punjab
Design and Synthesis of Sulfonium Derivatives: A Novel Class of α-Glucosidase Inhibitors with Potent In Vivo Antihyperglycemic Activities.
J Med Chem 66: 3484-3498 (2023)
China Pharmaceutical University
Bioisosteric replacement of 1H-1,2,3-triazole with 1H-tetrazole ring enhances anti-leukemic activity of (5-benzylthiazol-2-yl)benzamides.
Eur J Med Chem 250: (2023)
University of Lviv
Advances in the development of phosphodiesterase-4 inhibitors.
Eur J Med Chem 250: (2023)
Guangdong Academy of Sciences
Design, Synthesis, and Biological Evaluation of Bipyridazine Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.
J Med Chem 66: 3327-3347 (2023)
Fudan University
Targeting Melanocortin Receptors Using S
J Med Chem 66: 3273-3283 (2023)
Monash University (Parkville Campus)
Palladium-Catalyzed Synthesis, Acetylcholinesterase Inhibition, and Neuroprotective Activities of
J Nat Prod 86: 939-946 (2023)
Southwest Jiaotong University
Structure-based discovery of pyrazolamides as novel ERRγ inverse agonists.
Eur J Med Chem 250: (2023)
Chonnam National University
Targeting mycobacterial membranes and membrane proteins: Progress and limitations.
Bioorg Med Chem 81: (2023)
National Institute of Pharmaceutical Education and Research-Hyderabad
Structure optimization and discovery of novel compound for the treatment of insertion mutations within exon 20 of EGFR and HER2.
Bioorg Med Chem 81: (2023)
Nankai University
Discovery and Characterization of BAY-805, a Potent and Selective Inhibitor of Ubiquitin-Specific Protease USP21.
J Med Chem 66: 3431-3447 (2023)
Bayer
Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss.
J Med Chem 66: 3195-3211 (2023)
Pfizer
Structural Optimization of Fibroblast Growth Factor Receptor Inhibitors for Treating Solid Tumors.
J Med Chem 66: 3226-3249 (2023)
Shanghai Institute of Materia Medica
Discovery of Sibiriline derivatives as novel receptor-interacting protein kinase 1 inhibitors.
Eur J Med Chem 250: (2023)
China Pharmaceutical University
Design, synthesis and evaluation of nitric oxide releasing derivatives of 2,4-diaminopyrimidine as novel FAK inhibitors for intervention of metastatic triple-negative breast cancer.
Eur J Med Chem 250: (2023)
Central South University
Discovery of Potent DYRK2 Inhibitors with High Selectivity, Great Solubility, and Excellent Safety Properties for the Treatment of Prostate Cancer.
J Med Chem 66: 4215-4230 (2023)
China Pharmaceutical University
Discovery of Highly Potent and Selective Thyroid Hormone Receptor β Agonists for the Treatment of Nonalcoholic Steatohepatitis.
J Med Chem 66: 3284-3300 (2023)
Shanghai Institute of Materia Medica
Novel dithiocarbamates selectively inhibit 3CL protease of SARS-CoV-2 and other coronaviruses.
Eur J Med Chem 250: (2023)
Univ. Lille
Advances in the development of phosphodiesterase 7 inhibitors.
NA
Southern Medical University
4-(5-Amino-pyrazol-1-yl)benzenesulfonamide derivatives as novel multi-target anti-inflammatory agents endowed with inhibitory activity against COX-2, 5-LOX and carbonic anhydrase: Design, synthesis, and biological assessments.
Eur J Med Chem 250: (2023)
Damanhour University
Discovery of a Novel Series of Imidazopyrazine Derivatives as Potent SHP2 Allosteric Inhibitors.
ACS Med Chem Lett 14: 156-162 (2023)
IRBM
Discovery of Selective Aldehyde Dehydrogenase Inhibitors for the Treatment of Cancer.
ACS Med Chem Lett 14: 131-132 (2023)
Usona Institute
Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.
ACS Med Chem Lett 14: 199-210 (2023)
Ontario Institute for Cancer Research
A Quantum Mechanics-Based Method to Predict Intramolecular Hydrogen Bond Formation Reflecting P-glycoprotein Recognition.
ACS Med Chem Lett 14: 223-228 (2023)
Shionogi
Structure-Based Design of Glycosylated Oxytocin Analogues with Improved Selectivity and Antinociceptive Activity.
ACS Med Chem Lett 14: 163-170 (2023)
The University of Arizona
Inhibitors of Interleukin 4 Induced Protein 1 (IL4I1) as Potential Treatment for Cancer.
ACS Med Chem Lett 14: 127-128 (2023)
Therachem Research Medilab
Plasma Kallikrein Inhibitors as Potential Treatment for Diabetic Macular Edema, Retinal Vein Occlusion, Hereditary Angioedema and Other Related Diseases.
ACS Med Chem Lett 14: 129-130 (2023)
Therachem Research Medilab
Inhibition of HIV-1 Protease by a Boronic Acid with High Oxidative Stability.
ACS Med Chem Lett 14: 171-175 (2023)
Massachusetts Institute of Technology
Incorporation of an Isohexide Subunit Improves the Drug-like Properties of Bioactive Compounds.
ACS Med Chem Lett 14: 176-182 (2023)
Rutgers The State University of New Jersey
Design, Synthesis, and Bioevaluation of Pyrido[2,3-
ACS Med Chem Lett 14: 183-190 (2023)
Nanjing University of Chinese Medicine
Macrocyclic Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonists.
ACS Med Chem Lett 14: 191-198 (2023)
Pfizer
Pyrazole Ureas as Low Dose, CNS Penetrant Glucosylceramide Synthase Inhibitors for the Treatment of Parkinson's Disease.
ACS Med Chem Lett 14: 146-155 (2023)
Merck
Synthesis and structure-activity relationship of new nicotinamide phosphoribosyltransferase inhibitors with antitumor activity on solid and haematological cancer.
Eur J Med Chem 250: (2023)
Universidad De Sevilla
Recent advances on dual inhibitors targeting HIV reverse transcriptase associated polymerase and ribonuclease H.
NA
Armed Police Forces Hospital of Sichuan
A Medicinal Chemistry Perspective on Excitatory Amino Acid Transporter 2 Dysfunction in Neurodegenerative Diseases.
J Med Chem 66: 2330-2346 (2023)
King'S College London
Scaffold Hybrid of the Natural Product Tanshinone I with Piperidine for the Discovery of a Potent NLRP3 Inflammasome Inhibitor.
J Med Chem 66: 2946-2963 (2023)
Zhejiang University
Discovery of Novel
J Med Chem 66: 2681-2698 (2023)
China Pharmaceutical University
Design, Synthesis, and Biological Activity of Marinacarboline Analogues as STAT3 Pathway Inhibitors for Docetaxel-Resistant Triple-Negative Breast Cancer.
J Med Chem 66: 3106-3133 (2023)
Seoul National University
From (Tool)Bench to Bedside: The Potential of Necroptosis Inhibitors.
J Med Chem 66: 2361-2385 (2023)
The Walter and Eliza Hall Institute of Medical Research
Expanding role of CXCR2 and therapeutic potential of CXCR2 antagonists in inflammatory diseases and cancers.
Eur J Med Chem 250: (2023)
China Pharmaceutical University
Rational design and appraisal of selective Cdc2-Like kinase 1 (Clk1) inhibitors as novel autophagy inducers for the treatment of acute liver injury (ALI).
Eur J Med Chem 250: (2023)
West China Hospital of Sichuan University
Homologation of the Alkyl Side Chain of Antimitotic Phenyl 4-(2-Oxo-3-alkylimidazolidin-1-yl)benzenesulfonate Prodrugs Selectively Targeting CYP1A1-Expressing Breast Cancers Improves Their Stability in Rodent Liver Microsomes.
J Med Chem 66: 2477-2497 (2023)
University Laval
Design, synthesis and evaluation of the novel chalcone derivatives with 2,2-dimethylbenzopyran as HIF-1 inhibitors that possess anti-angiogenic potential.
Eur J Med Chem 250: (2023)
Shenyang Pharmaceutical University
Design, Synthesis, and Biological Evaluation of a Potent Dual EZH2-BRD4 Inhibitor for the Treatment of Some Solid Tumors.
J Med Chem 66: 2646-2662 (2023)
Sichuan University
Various strategies for developing APOBEC3G protectors to circumvent human immunodeficiency virus type 1.
Eur J Med Chem 250: (2023)
Zhejiang Normal University
Synthesis and structure-activity optimization of 7-azaindoles containing aza-β-amino acids targeting the influenza PB2 subunit.
Eur J Med Chem 250: (2023)
Zhejiang University
Synthesis and biological evaluation of 2,5-disubstituted furan derivatives containing 1,3-thiazole moiety as potential α-glucosidase inhibitors.
Bioorg Med Chem Lett 83: (2023)
South China Agricultural University
Tetrazole-based inhibitors of the bacterial enzyme N-succinyl-l,l-2,6-diaminopimelic acid desuccinylase as potential antibiotics.
Bioorg Med Chem Lett 83: (2023)
Loyola University Chicago
The structure-based optimization of 3-substituted indolin-2-one derivatives as potent and isoform-selective c-Jun N-terminal kinase 3 (JNK3) inhibitors and biological evaluation.
Eur J Med Chem 250: (2023)
Peking University
Discovery of unglycosylated indolocarbazoles as ROCK2 isoform-selective inhibitors for the treatment of breast cancer metastasis.
Eur J Med Chem 250: (2023)
Zhejiang University
Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer.
J Med Chem 66: 2851-2864 (2023)
Jinan University
Identification of specific carbonic anhydrase inhibitors
RSC Med Chem 14: 144-153 (2023)
Czech Academy of Sciences
Design, synthesis and biological evaluation of pyrazolo[3,4-
RSC Med Chem 14: 85-102 (2023)
Shenyang Pharmaceutical University
Advances in research on 3C-like protease (3CL
RSC Med Chem 14: 9-21 (2023)
Huaqiao University
Synthesis and bioactive evaluation of
RSC Med Chem 14: 113-121 (2023)
Guangxi University
It's ok to be outnumbered - sub-stoichiometric modulation of homomeric protein complexes.
RSC Med Chem 14: 22-46 (2023)
Genentech
Application and synthesis of thiazole ring in clinically approved drugs.
Eur J Med Chem 250: (2023)
Zhengzhou University
The Development and Design Strategy of Leucine-Rich Repeat Kinase 2 Inhibitors: Promising Therapeutic Agents for Parkinson's Disease.
J Med Chem 66: 2282-2307 (2023)
China Pharmaceutical University
Alkyne Derivatives of SARS-CoV-2 Main Protease Inhibitors Including Nirmatrelvir Inhibit by Reacting Covalently with the Nucleophilic Cysteine.
J Med Chem 66: 2663-2680 (2023)
University of Oxford
Discovery of a Series of Substituted 1
J Med Chem 66: 2877-2892 (2023)
Janssen Research & Development
Discovery of Novel Human Constitutive Androstane Receptor Agonists with the Imidazo[1,2-
J Med Chem 66: 2422-2456 (2023)
Czech Academy of Sciences
2,6-diazaspiro[3.4]octan-7-one derivatives as potent sigma-1 receptor antagonists that enhanced the antinociceptive effect of morphine and rescued morphine tolerance.
Eur J Med Chem 249: (2023)
Xuzhou Medical University
Thioxanthenone-based derivatives as multitarget therapeutic leads for Alzheimer's disease.
Eur J Med Chem 250: (2023)
University of Genoa
Tuning liver pyruvate kinase activity up or down with a new class of allosteric modulators.
Eur J Med Chem 250: (2023)
University of Gothenburg
Amide containing NBTI antibacterials with reduced hERG inhibition, retained antimicrobial activity against gram-positive bacteria and in vivo efficacy.
Eur J Med Chem 250: (2023)
University of Ljubljana
Discovery of 2-(3-Benzamidopropanamido)thiazole-5-carboxylate Inhibitors of the Kinesin HSET (KIFC1) and the Development of Cellular Target Engagement Probes.
J Med Chem 66: 2622-2645 (2023)
Institute of Cancer Research
Improvement of the Metabolic Stability of GPR88 Agonist RTI-13951-33: Design, Synthesis, and Biological Evaluation.
J Med Chem 66: 2964-2978 (2023)
Research Triangle Institute
Development of Furanopyrimidine-Based Orally Active Third-Generation EGFR Inhibitors for the Treatment of Non-Small Cell Lung Cancer.
J Med Chem 66: 2566-2588 (2023)
National Health Research Institutes
Discovery of Novel PTP1B Inhibitors with Once-Weekly Therapeutic Potential for Type 2 Diabetes: Design, Synthesis, and
J Med Chem 66: 3030-3044 (2023)
Qingdao University
Novel Strategy To Inhibit Transthyretin Amyloidosis via the Synergetic Effect of Chemoselective Acylation and Noncovalent Inhibitor Release.
J Med Chem 66: 2893-2903 (2023)
Chungnam National University
Strategies of Targeting CK2 in Drug Discovery: Challenges, Opportunities, and Emerging Prospects.
J Med Chem 66: 2257-2281 (2023)
Sichuan University
Evaluation of darunavir-derived HIV-1 protease inhibitors incorporating P2' amide-derivatives: Synthesis, biological evaluation and structural studies.
Bioorg Med Chem Lett 83: (2023)
Purdue University
Discovery of novel and bioavailable histone deacetylases and cyclin-dependent kinases dual inhibitor to impair the stemness of leukemia cells.
Eur J Med Chem 249: (2023)
Nankai University
A novel pan-selective bromodomain inhibitor for epigenetic drug design.
Eur J Med Chem 249: (2023)
Albert-Ludwigs-Universit£T Freiburg
Discovery of potent Plasmodium falciparum protein kinase 6 (PfPK6) inhibitors with a type II inhibitor pharmacophore.
Eur J Med Chem 249: (2023)
University of North Carolina at Chapel Hill
Discovery of a Potent and Selective STAT5 PROTAC Degrader with Strong Antitumor Activity
J Med Chem 66: 2717-2743 (2023)
University of Michigan
Development of Human Carbonic Anhydrase II Heterobifunctional Degraders.
J Med Chem 66: 2789-2803 (2023)
University of California
Structure-Activity Relationship of Novel Pyrimidine Derivatives with Potent Inhibitory Activities against
J Med Chem 66: 2699-2716 (2023)
Sichuan University
Discovery of CZS-241: A Potent, Selective, and Orally Available Polo-Like Kinase 4 Inhibitor for the Treatment of Chronic Myeloid Leukemia.
J Med Chem 66: 2396-2421 (2023)
Shenyang Pharmaceutical University
Treatment of allergy: Overview of synthetic anti-allergy small molecules in medicinal chemistry.
Eur J Med Chem 249: (2023)
Zhejiang Sci-Tech University
PKM2/PDK1 dual-targeted shikonin derivatives restore the sensitivity of EGFR-mutated NSCLC cells to gefitinib by remodeling glucose metabolism.
Eur J Med Chem 249: (2023)
Nanjing University
Tackling multidrug-resistant Staphylococcus aureus by natural products and their analogues acting as NorA efflux pump inhibitors.
Bioorg Med Chem 80: (2023)
National Institute of Pharmaceutical Education and Research-Hyderabad
Identification of M4205─A Highly Selective Inhibitor of KIT Mutations for Treatment of Unresectable Metastatic or Recurrent Gastrointestinal Stromal Tumors.
J Med Chem 66: 2386-2395 (2023)
Merck Healthcare
Discovery of a Novel Potent and Selective HSD17B13 Inhibitor, BI-3231, a Well-Characterized Chemical Probe Available for Open Science.
J Med Chem 66: 2832-2850 (2023)
Boehringer Ingelheim Pharma
Triazole-fused pyrimidines in target-based anticancer drug discovery.
Eur J Med Chem 249: (2023)
Zhenzhou University
Small molecule inhibitors of intestinal epithelial anion exchanger SLC26A3 (DRA) with a luminal, extracellular site of action.
Eur J Med Chem 249: (2023)
University of California San Francisco
Developments of PROTACs technology in immune-related diseases.
Eur J Med Chem 249: (2023)
The Affiliated Hospital of Qingdao University
Optimized M24B Aminopeptidase Inhibitors for CARD8 Inflammasome Activation.
J Med Chem 66: 2589-2607 (2023)
Memorial Sloan Kettering Cancer Center
Structure-Based Design of Novel Alkynyl Thio-Benzoxazepinone Receptor-Interacting Protein Kinase-1 Inhibitors: Extending the Chemical Space from the Allosteric to ATP Binding Pockets.
J Med Chem 66: 3073-3087 (2023)
Ningxia Medical University
Selective Covalent Targeting of Pyruvate Kinase M2 Using Arsenous Warheads.
J Med Chem 66: 2608-2621 (2023)
Chinese Academy of Sciences
Discovery of orally bioavailable inhibitors of MALT1 with in vivo activity for psoriasis.
Bioorg Med Chem Lett 82: (2023)
Toray Industries
Discovery of Highly Potent and BMPR2-Selective Kinase Inhibitors Using DNA-Encoded Chemical Library Screening.
J Med Chem 66: 2143-2160 (2023)
Baylor College of Medicine
Discovery of novel 2-hydroxyl-4-benzyloxybenzyl aniline derivatives as potential multifunctional agents for the treatment of Parkinson's disease.
Eur J Med Chem 249: (2023)
North Sichuan Medical College
Novel S1R agonists counteracting NMDA excitotoxicity and oxidative stress: A step forward in the discovery of neuroprotective agents.
Eur J Med Chem 249: (2023)
University of Pavia
Design, synthesis, docking, and biochemical characterization of non-nucleoside SARS-CoV-2 RdRp inhibitors.
Bioorg Med Chem 80: (2023)
Istituto Italiano Di Tecnologia
Application of Novel Degraders Employing Autophagy for Expediting Medicinal Research.
J Med Chem 66: 1700-1711 (2023)
Chengdu University of Traditional Chinese Medicine
1,2,4-Amino-triazine derivatives as pyruvate dehydrogenase kinase inhibitors: Synthesis and pharmacological evaluation.
Eur J Med Chem 249: (2023)
University of Palermo
Discovery of aromatic 2-(3-(methylcarbamoyl) guanidino)-N-aylacetamides as highly potent chitinase inhibitors.
Bioorg Med Chem 80: (2023)
China Agricultural University
Insight into non-nucleoside triazole-based systems as viral polymerases inhibitors.
Eur J Med Chem 249: (2023)
University of Palermo
Design, synthesis and in vitro biological evaluation of 2-aminopyridine derivatives as novel PI3Kδ inhibitors for hematological cancer.
Bioorg Med Chem Lett 82: (2023)
Fudan University
Design, synthesis, and biological evaluation of novel N-Benzyl piperidine derivatives as potent HDAC/AChE inhibitors for Alzheimer's disease.
Bioorg Med Chem 80: (2023)
Shandong University
2-Anilino-4-(1-methyl-1H-pyrazol-4-yl)pyrimidine-derived CDK2 inhibitors as anticancer agents: Design, synthesis & evaluation.
Bioorg Med Chem 80: (2023)
University of South Australia
Design of an Ultralow Molecular Weight Heparin That Resists Heparanase Biodegradation.
J Med Chem 66: 2194-2203 (2023)
Harvard Medical School
"Hit" to lead optimization and chemoinformatic studies for a new series of Autotaxin inhibitors.
Eur J Med Chem 249: (2023)
Bioinnovation Institute
Discovery, synthesis and mechanism study of 2,3,5-substituted [1,2,4]-thiadiazoles as covalent inhibitors targeting 3C-Like protease of SARS-CoV-2.
Eur J Med Chem 249: (2023)
Shanghaitech University
Screening through Lead Optimization of High Affinity, Allosteric Cyclin-Dependent Kinase 2 (CDK2) Inhibitors as Male Contraceptives That Reduce Sperm Counts in Mice.
J Med Chem 66: 1928-1940 (2023)
University of Minnesota
Structure-Based Optimization of 2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: Exploiting the Tolerant Regions of the Non-Nucleoside Reverse Transcriptase Inhibitors' Binding Pocket.
J Med Chem 66: 2102-2115 (2023)
Shandong University
Integrating a phenotypic screening with a structural simplification strategy to identify 4-phenoxy-quinoline derivatives to potently disrupt the mitotic localization of Aurora kinase B.
Bioorg Med Chem 80: (2023)
Chengdu Anticancer Bioscience
Discovery and pharmacological characterization of a novel benzimidazole TRPV4 antagonist with cyanocyclobutyl moiety.
Eur J Med Chem 249: (2023)
Beijing Institute of Pharmacology and Toxicology
Discovery of new, highly potent and selective inhibitors of BuChE - design, synthesis, in vitro and in vivo evaluation and crystallography studies.
Eur J Med Chem 249: (2023)
Jagiellonian University Medical College
Development of novel pyrazole, imidazo[1,2-b]pyrazole, and pyrazolo[1,5-a]pyrimidine derivatives as a new class of COX-2 inhibitors with immunomodulatory potential.
Eur J Med Chem 249: (2023)
Al-Azhar University
Recent Advances on Small-Molecule Bromodomain-Containing Histone Acetyltransferase Inhibitors.
J Med Chem 66: 1678-1699 (2023)
Sichuan University
Discovery of AXL Degraders with Improved Potencies in Triple-Negative Breast Cancer (TNBC) Cells.
J Med Chem 66: 1873-1891 (2023)
Jinan University
Design and Synthesis of Orally Active Quinolyl Pyrazinamides as Sigma 2 Receptor Ligands for the Treatment of Pancreatic Cancer.
J Med Chem 66: 1990-2019 (2023)
University of Michigan
METTL3 from Target Validation to the First Small-Molecule Inhibitors: A Medicinal Chemistry Journey.
J Med Chem 66: 1654-1677 (2023)
Sapienza University of Rome
Discovery of a Novel Covalent EZH2 Inhibitor Based on Tazemetostat Scaffold for the Treatment of Ovarian Cancer.
J Med Chem 66: 1725-1741 (2023)
Sichuan University
Discovery of indole-piperazine derivatives as selective histone deacetylase 6 inhibitors with neurite outgrowth-promoting activities and neuroprotective activities.
Bioorg Med Chem Lett 81: (2023)
Northwest A&F University
Design and synthesis of novel orexin 2 receptor agonists with a 1,3,5‑trioxazatriquinane skeleton.
Bioorg Med Chem Lett 82: (2023)
University of Tsukuba
ATP-competitive inhibitors of human DNA topoisomerase IIα with improved antiproliferative activity based on N-phenylpyrrolamide scaffold.
Eur J Med Chem 249: (2023)
University of Ljubljana
Structure-Directed Discovery of Potent Soluble Epoxide Hydrolase Inhibitors for the Treatment of Inflammatory Diseases.
J Med Chem 66: 2979-3009 (2023)
Shenyang Pharmaceutical University
SAR study of piperidine derivatives as inhibitors of 1,4-dihydroxy-2-naphthoate isoprenyltransferase (MenA) from Mycobacterium tuberculosis.
Eur J Med Chem 249: (2023)
University of Minnesota
A-ring-fused pyrazoles of dihydrotestosterone targeting prostate cancer cells via the downregulation of the androgen receptor.
Eur J Med Chem 249: (2023)
Palacky University
Novel neuroprotective pyromeconic acid derivatives with concurrent anti-Aβ deposition, anti-inflammatory, and anti-oxidation properties for treatment of Alzheimer's disease.
Eur J Med Chem 248: (2023)
Fujian Medical University
Discovery, Characterization, and Engineering of LvIC, an α4/4-Conotoxin That Selectively Blocks Rat α6/α3β4 Nicotinic Acetylcholine Receptors.
J Med Chem 66: 2020-2031 (2023)
Guangxi University
Hybrids of polyphenolic/quinone acids, the potential preventive and therapeutic drugs for PD: Disaggregate α-Syn fibrils, inhibit inclusions, and repair damaged neurons in mice.
Eur J Med Chem 249: (2023)
Zhengzhou University
Annual review of KRAS inhibitors in 2022.
Eur J Med Chem 249: (2023)
Zhengzhou University
Synthetic α-glucosidase inhibitors as promising anti-diabetic agents: Recent developments and future challenges.
Eur J Med Chem 249: (2023)
Quaid-I-Azam University
Development of fluorophore labeled or biotinylated anticancer small molecule NSC243928.
Bioorg Med Chem 79: (2023)
University of South Carolina
Optimization of BAX trigger site activator BTSA1 with improved antitumor potency and in vitro ADMET properties.
Eur J Med Chem 248: (2023)
Shenyang Pharmaceutical University
Structure-activity relationship (SAR) studies on substituted N-(pyridin-3-yl)-2-amino-isonicotinamides as highly potent and selective glycogen synthase kinase-3 (GSK-3) inhibitors.
Bioorg Med Chem Lett 81: (2023)
Bristol-Myers Squibb
Telomerase: A prominent oncological target for development of chemotherapeutic agents.
Eur J Med Chem 249: (2023)
Nirma University
Privileged heterocycles for DNA-encoded library design and hit-to-lead optimization.
Eur J Med Chem 248: (2023)
Chinese Academy of Sciences
Optimized Ebselen-Based Inhibitors of Bacterial Ureases with Nontypical Mode of Action.
J Med Chem 66: 2054-2063 (2023)
Wroclaw University
Dopamine D
J Med Chem 66: 1809-1834 (2023)
National Institute On Drug Abuse?Intramural Research Program
Synthesis and discovery of Baylis-Hillman adducts as potent and selective thioredoxin reductase inhibitors for cancer treatment.
Bioorg Med Chem 79: (2023)
Lanzhou Jiaotong University
N-adamantyl-anthranil amide derivatives: New selective ligands for the cannabinoid receptor subtype 2 (CB2R).
Eur J Med Chem 248: (2023)
University of The Studies of Bari "Aldo Moro
Thorectidiol A Isolated from the Marine Sponge
J Nat Prod 86: 582-588 (2023)
University of British Columbia
Discovery and Characterization of the Topical Soft JAK Inhibitor CEE321 for Atopic Dermatitis.
J Med Chem 66: 2161-2168 (2023)
Novartis
Potent and Selective Biaryl Amide Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).
ACS Med Chem Lett 14: 116-122 (2023)
Incyte Research Institute
Structural Characterization of Thiadiazolesulfonamide Inhibitors Bound to
ACS Med Chem Lett 14: 103-109 (2023)
Purdue University
Using Imidazo[2,1-
ACS Med Chem Lett 14: 83-91 (2023)
Ocean University of China and Laboratory For Marine Drugs and Bioproducts
Synthesis of Novel Kidney-Type Glutaminase Allosteric Inhibitors Targeting the Critical Lys-320 Residue.
ACS Med Chem Lett 14: 11-17 (2023)
Zhejiang University
Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure-Activity Relationship.
ACS Med Chem Lett 14: 18-25 (2023)
IQM-CSIC
Discovery of Paltusotine (CRN00808), a Potent, Selective, and Orally Bioavailable Non-peptide SST2 Agonist.
ACS Med Chem Lett 14: 66-74 (2023)
Crinetics Pharmaceuticals
In the Quest for Potent and Selective Malic Enzyme 3 Inhibitors for the Treatment of Pancreatic Ductal Adenocarcinoma.
ACS Med Chem Lett 14: 41-50 (2023)
Sun Pharma Advanced Research Company
Discovery of Pyrazolopyridine Derivatives as HPK1 Inhibitors.
ACS Med Chem Lett 14: 5-10 (2023)
Incyte Research Institute
Identification of 2-Aminoacyl-1,3,4-thiadiazoles as Prostaglandin E
ACS Med Chem Lett 14: 26-34 (2023)
University of Salerno
Visible-Light-Controlled Histone Deacetylase Inhibitors for Targeted Cancer Therapy.
J Med Chem 66: 1909-1927 (2023)
Institute for Advanced Chemistry of Catalonia (IQAC-CSIC)
Divergent reactivity of usnic acid and evaluation of its derivatives for antiproliferative activity against cancer cells.
Bioorg Med Chem 79: (2023)
Australian National University
Identification of Natural Products Inhibiting SARS-CoV-2 by Targeting Viral Proteases: A Combined in Silico and in Vitro Approach.
J Nat Prod 86: 264-275 (2023)
University of Vienna
Discovery of Novel Indazole Chemotypes as Isoform-Selective JNK3 Inhibitors for the Treatment of Parkinson's Disease.
J Med Chem 66: 1273-1300 (2023)
Sichuan University
Design, synthesis of novel benzimidazole derivatives as ENL inhibitors suppressing leukemia cells viability via downregulating the expression of MYC.
Eur J Med Chem 248: (2023)
Nanchang University
Synthesis and biological evaluation of novel N-benzyltriazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors.
Bioorg Med Chem 79: (2023)
Sungkyunkwan University
Targeting Death-Associated Protein Kinases for Treatment of Human Diseases: Recent Advances and Future Directions.
J Med Chem 66: 1112-1136 (2023)
Southwest Jiaotong University
Structural Modification and Pharmacological Evaluation of Substituted Quinoline-5,8-diones as Potent NSD2 Inhibitors.
J Med Chem 66: 1634-1651 (2023)
Shanghai Jiao Tong University
Ras superfamily GTPase activating proteins in cancer: Potential therapeutic targets?
Eur J Med Chem 248: (2023)
National Clinical Research Center For Geriatrics
New amidine-benzenesulfonamides as iNOS inhibitors for the therapy of the triple negative breast cancer.
Eur J Med Chem 248: (2023)
University of Granada
Identification of pyrimidinyl piperazines as non-iminosugar glucocerebrosidase (GCase) pharmacological chaperones.
Bioorg Med Chem Lett 81: (2023)
Eisai
Design and synthesis of 6-methylpyridin-2-one derivatives as novel and potent GluN2A positive allosteric modulators for the treatment of cognitive impairment.
Bioorg Med Chem 79: (2023)
Takeda Pharmaceutical
Development and therapeutic potential of adaptor-associated kinase 1 inhibitors in human multifaceted diseases.
Eur J Med Chem 248: (2023)
Sichuan Univiersity
Hybrids of delavirdine and piperdin-4-yl-aminopyrimidines (DPAPYs) as potent HIV-1 NNRTIs: Design, synthesis and biological activities.
Eur J Med Chem 248: (2023)
Wuhan Institute of Technology
8-Amide and 8-carbamate substitution patterns as modulators of 7-hydroxy-4-methylcoumarin's antidepressant profile: Synthesis, biological evaluation and docking studies.
Eur J Med Chem 248: (2023)
Universidade do Porto (CIQUP)
Design, synthesis and anti-AD effects of dual inhibitor targeting glutaminyl cyclase/GSK-3β.
Eur J Med Chem 248: (2023)
Shenzhen University
Design, synthesis, and evaluation of pyrido.[3,4-b]pyrazin-2(1H)-one derivatives as potent FLT3 inhibitors.
Bioorg Med Chem 79: (2023)
Zhejiang University
Synthesis of pyrrolo[3,2-d]pyrimidineone derivatives as novel FXa inhibitors.
Bioorg Med Chem Lett 80: (2023)
Nanjing Zhongrui Pharmaceutical Co.
Investigation of morpholine isosters for the development of a potent, selective and metabolically stable mTOR kinase inhibitor.
Eur J Med Chem 248: (2023)
University of Basel
Exploiting HOPNO-dicopper center interaction to development of inhibitors for human tyrosinase.
Eur J Med Chem 248: (2023)
University of Grenoble Alpes
Design, synthesis, and biological activity studies on benzimidazole derivatives targeting myeloperoxidase.
Eur J Med Chem 248: (2023)
Izmir Katip Celebi University
Synthesis and structure-activity relationships of N - (3 - (1H-imidazol-2-yl) phenyl) - 3-phenylpropionamide derivatives as a novel class of covalent inhibitors of p97/VCP ATPase.
Eur J Med Chem 248: (2023)
Chinese Academy of Medical Sciences and Peking Union Medical College
Discovery and Hit-to-Lead Optimization of Benzothiazole Scaffold-Based DNA Gyrase Inhibitors with Potent Activity against
J Med Chem 66: 1380-1425 (2023)
University of Ljubljana
Hypouricemic Actions of the Pericarp of Mangosteen
J Nat Prod 86: 24-33 (2023)
Kunming Medical University
Structure-Activity Relationship Studies of Venglustat on NTMT1 Inhibition.
J Med Chem 66: 1601-1615 (2023)
Purdue University
Rationally designed donepezil-based hydroxamates modulate Sig-1R and HDAC isoforms to exert anti-glioblastoma effects.
Eur J Med Chem 248: (2023)
Taipei Medical University
Structure-Activity Relationship Studies of Antimalarial
J Med Chem 66: 1484-1508 (2023)
Weill Cornell Medicine
Discovery of Novel 3-Phenylpiperidine Derivatives Targeting the β-Catenin/B-Cell Lymphoma 9 Interaction as a Single Agent and in Combination with the Anti-PD-1 Antibody for the Treatment of Colorectal Cancer.
J Med Chem 66: 1349-1379 (2023)
Fudan University
Discovery of the GSH responsive "Y-PROTACs" targeting ALK and CDK4/6 as a potential treatment for cancer.
Eur J Med Chem 248: (2023)
West China Hospital of Sichuan University
Inhibitors of ABCG2-mediated multidrug resistance: Lead generation through computer-aided drug design.
Eur J Med Chem 248: (2023)
University of Perugia
First-in-Class Dual Hybrid Carbonic Anhydrase Inhibitors and Transient Receptor Potential Vanilloid 1 Agonists Revert Oxaliplatin-Induced Neuropathy.
J Med Chem 66: 1616-1633 (2023)
University of Florence
Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia.
J Med Chem 66: 1157-1171 (2023)
Merck
BET-HDAC Dual Inhibitors for Combinational Treatment of Breast Cancer and Concurrent Candidiasis.
J Med Chem 66: 1239-1253 (2023)
Second Military Medical University
Searching for Novel Noncovalent Nuclear Export Inhibitors through a Drug Repurposing Approach.
J Med Chem 66: 1574-1582 (2023)
Sichuan University
Fragment-to-Lead Medicinal Chemistry Publications in 2021.
J Med Chem 66: 1137-1156 (2023)
Astex Pharmaceuticals
Design, synthesis and biological evaluation of KRAS
Bioorg Med Chem 78: (2023)
China Pharmaceutical University
Computer-aided identification, synthesis, and biological evaluation of DNA polymerase η inhibitors for the treatment of cancer.
Eur J Med Chem 248: (2023)
Istituto Italiano Di Tecnologia
Development of a series of quinazoline-2,5-diamine derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors.
Eur J Med Chem 248: (2023)
Shanghai Institute of Materia Medica
Computational, in vitro and radiation-based in vivo studies on acetamide quinazolinone derivatives as new proposed purine nucleoside phosphorylase inhibitors for breast cancer.
Eur J Med Chem 248: (2023)
National Center for Radiation Research and Technology
Pleiotropic effects of a mitochondrion-targeted glutathione reductase inhibitor on restraining tumor cells.
Eur J Med Chem 248: (2023)
The Affiliated Hospital of Qingdao University
Fluorescent and theranostic probes for imaging nicotinamide phosphoribosyl transferase (NAMPT).
Eur J Med Chem 248: (2023)
Second Military Medical University (Naval Medical University)
Discovery of Highly Selective Inhibitors of the Human Constitutive Proteasome β5c Chymotryptic Subunit.
J Med Chem 66: 1172-1185 (2023)
Weill Cornell Medicine
Dual degradation mechanism of GPX4 degrader in induction of ferroptosis exerting anti-resistant tumor effect.
Eur J Med Chem 247: (2023)
Peking University
Hybrid molecules combining GABA-A and serotonin 5-HT
Eur J Med Chem 247: (2023)
Jagiellonian University Medical College
Dual inhibitors of ASK1 and PDK1 kinases: Design, synthesis, molecular docking and mechanism studies of N-benzyl pyridine-2-one containing derivatives as anti-fibrotic agents.
Eur J Med Chem 247: (2023)
Central South University
Application of deep generative model for design of Pyrrolo[2,3-d] pyrimidine derivatives as new selective TANK binding kinase 1 (TBK1) inhibitors.
Eur J Med Chem 247: (2023)
Jinan University
Nanomolar β-glucosidase and β-galactosidase inhibition by enantiomeric α-1-C-alkyl-1,4-dideoxy-1,4-imino-arabinitol derivatives.
Eur J Med Chem 247: (2023)
Chinese Academy of Sciences
Design, synthesis, and biological evaluation of quinoxalinone derivatives as potent BRD4 inhibitors.
Bioorg Med Chem 78: (2023)
Lanzhou University
Design, synthesis and antitumor activity of novel thiophene- triazine derivatives bearing arylurea unit as potent PI3K/mTOR inhibitorss.
Bioorg Med Chem 78: (2023)
Shenyang Pharmaceutical University
Targeting ecto-5'-nucleotidase: A comprehensive review into small molecule inhibitors and expression modulators.
Eur J Med Chem 247: (2023)
Federal University of Rio Grande Do Sul
Design, synthesis and biological evaluation of quercetin derivatives as novel β-catenin/B-cell lymphoma 9 protein-protein interaction inhibitors.
Eur J Med Chem 247: (2023)
Fudan University
Deciphering Nonbioavailable Substructures Improves the Bioavailability of Antidepressants by Serotonin Transporter.
J Med Chem 66: 371-383 (2023)
Central China Normal University
Dual Nicotinamide Phosphoribosyltransferase (NAMPT) and Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors for the Treatment of Drug-Resistant Nonsmall-Cell Lung Cancer.
J Med Chem 66: 1027-1047 (2023)
China Pharmaceutical University
Discovery of TP0597850: A Selective, Chemically Stable, and Slow Tight-Binding Matrix Metalloproteinase-2 Inhibitor with a Phenylbenzamide-Pentapeptide Hybrid Scaffold.
J Med Chem 66: 822-836 (2023)
Taisho Pharmaceutical Co.
Discovery of Novel Drug-like PHGDH Inhibitors to Disrupt Serine Biosynthesis for Cancer Therapy.
J Med Chem 66: 285-305 (2023)
Innovation Research Institute of Traditional Chinese Medicine
Synthesis and pharmacological validation of a novel radioligand for the orphan GPR88 receptor.
Bioorg Med Chem Lett 80: (2023)
Research Triangle Institute
Synthesis and evaluation of a new class of MIF-inhibitors in activated macrophage cells and in experimental septic shock in mice.
Eur J Med Chem 247: (2023)
University of Pecs
Pseudo-irreversible butyrylcholinesterase inhibitors: Structure-activity relationships, computational and crystallographic study of the N-dialkyl O-arylcarbamate warhead.
Eur J Med Chem 247: (2023)
University of Ljubljana
Function-oriented synthesis of Imidazo[1,2-a]pyrazine and Imidazo[1,2-b]pyridazine derivatives as potent PI3K/mTOR dual inhibitors.
Eur J Med Chem 247: (2023)
East China Normal University
Structure-activity relationship and biological evaluation of xanthine derivatives as PCSK9 inhibitors for the treatment of atherosclerosis.
Eur J Med Chem 247: (2023)
Peking Union Medical College
Development of potent and selective degraders of PI5P4Kγ.
Eur J Med Chem 247: (2023)
Stanford University
Design and synthesis of improved active-site SHP2 inhibitors with anti-breast cancer cell effects.
Eur J Med Chem 247: (2023)
West Virginia University
Mechanistic Insight of Synthesized 1,4-Dihydropyridines as an Antidiabetic Sword against Reactive Oxygen Species.
J Med Chem 66: 991-1010 (2023)
Tanta University
Indole Derivatives as New Structural Class of Potent and Antiproliferative Inhibitors of Monocarboxylate Transporter 1 (MCT1; SLC16A1).
J Med Chem 66: 657-676 (2023)
Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management
Fine-tuning of nitrogen-containing bisphosphonate esters that potently induce degradation of HMG-CoA reductase.
Bioorg Med Chem 78: (2023)
Tokyo University of Science
Dual functional antioxidant and butyrylcholinesterase inhibitors for the treatment of Alzheimer's disease: Design, synthesis and evaluation of novel melatonin-alkylbenzylamine hybrids.
Bioorg Med Chem 78: (2023)
Jiangxi University of Chinese Medicine
Discovery of novel 5-methoxybenzothiophene hydrazides as metabolically stable Clk1 inhibitors with high potency and unprecedented Clk1 isoenzyme selectivity.
Eur J Med Chem 247: (2023)
German University In Cairo
Structure-Based Design of the Indole-Substituted Triazolopyrimidines as New EED-H3K27me3 Inhibitors for the Treatment of Lymphoma.
J Med Chem 66: 1063-1081 (2023)
Zhengzhou University
Novel Small-Molecule PD-L1 Inhibitor Induces PD-L1 Internalization and Optimizes the Immune Microenvironment.
J Med Chem 66: 2064-2083 (2023)
China Pharmaceutical University
Identification of 2,4,5-trisubstituted-2,4-dihydro-3H-1,2,4-triazol-3-one-based small molecules as selective BRD9 binders.
Eur J Med Chem 247: (2023)
University of Salerno
Current scenario of quinolone hybrids with potential antibacterial activity against ESKAPE pathogens.
Eur J Med Chem 247: (2023)
Shandong University
Identification of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
Eur J Med Chem 247: (2023)
Shandong University
Design, synthesis, in vitro - In vivo biological evaluation of novel thiazolopyrimidine compounds as antileishmanial agent with PTR1 inhibition.
Eur J Med Chem 247: (2023)
Izmir Katip Celebi University
Wiskostatin and other carbazole scaffolds as off target inhibitors of dynamin I GTPase activity and endocytosis.
Eur J Med Chem 247: (2023)
The University of Newcastle
Physachenolide C is a Potent, Selective BET Inhibitor.
J Med Chem 66: 913-933 (2023)
University of Arizona
Discovery of the Potent and Highly Selective PARP7 Inhibitor as a Novel Immunotherapeutic Agent for Tumors.
J Med Chem 66: 473-490 (2023)
China Pharmaceutical University
Targeted Protein Degradation Induced by HEMTACs Based on HSP90.
J Med Chem 66: 733-751 (2023)
Shandong University
Synthetic Strategies for Improving Solubility: Optimization of Novel Pyrazolo[1,5-
J Med Chem 66: 413-434 (2023)
Yonsei University
Discovery of DS-9300: A Highly Potent, Selective, and Once-Daily Oral EP300/CBP Histone Acetyltransferase Inhibitor.
J Med Chem 66: 695-715 (2023)
Daiichi Sankyo Co.
Bivalent dopamine agonists with co-operative binding and functional activities at dopamine D2 receptors, modulate aggregation and toxicity of alpha synuclein protein.
Bioorg Med Chem 78: (2023)
Wayne State University
Inhibition of the Ubiquitin Transfer Cascade by a Peptidomimetic Foldamer Mimicking the E2 N-Terminal Helix.
J Med Chem 66: 491-502 (2023)
Georgia State University
PROTACS: A technology with a gold rush-like atmosphere.
Eur J Med Chem 247: (2023)
China Pharmaceutical University
Development of highly potent and specific AKR1C3 inhibitors to restore the chemosensitivity of drug-resistant breast cancer.
Eur J Med Chem 247: (2023)
China Pharmaceutical University
Cyclization strategy leads to highly potent Bromodomain and extra-terminal (BET) Bromodomain inhibitors for the treatment of acute liver injury.
Eur J Med Chem 247: (2023)
Fudan University
Design, synthesis and evaluation of antitumor activity of selective PRMT6 inhibitors.
Eur J Med Chem 247: (2023)
Sichuan University
Modes of action insights from the crystallographic structures of retinoic acid receptor-related orphan receptor-γt (RORγt).
Eur J Med Chem 247: (2023)
Fudan University
The discovery of 3,3-dimethyl-1,2,3,4-tetrahydroquinoxaline-1-carboxamides as AMPD2 inhibitors with a novel mechanism of action.
Bioorg Med Chem Lett 80: (2023)
Japan Tobacco
Discovery of small-molecule protein stabilizers toward exogenous alpha-l-iduronidase to reduce the accumulated heparan sulfate in mucopolysaccharidosis type I cells.
Eur J Med Chem 247: (2023)
Genomics Research Center
Discovery of Highly Potent Nicotinamide Phosphoribosyltransferase Degraders for Efficient Treatment of Ovarian Cancer.
J Med Chem 66: 1048-1062 (2023)
Second Military Medical University
Selective Inhibition of Organic Cation Transporter 1 by Benzoylpaeoniflorin Attenuates Hepatic Lipid Accumulation through AMPK Activation.
J Nat Prod 86: 191-198 (2023)
Tianjin University
Optical-Controlled Kinetic Switch: Fine-Tuning of the Residence Time of an Antagonist Binding to the Vasopressin V
J Med Chem 66: 1454-1466 (2023)
Xuzhou Medical University
Discovery of High-Affinity Small-Molecule Binders of the Epigenetic Reader YEATS4.
J Med Chem 66: 460-472 (2023)
Pfizer
Small-Molecule Cyanamide Pan-TEAD·YAP1 Covalent Antagonists.
J Med Chem 66: 266-284 (2023)
Indiana University
Advanced approaches of developing targeted covalent drugs.
RSC Med Chem 13: 1460-1475 (2022)
College of Pharmacy
Pyrazolines as potential anti-Alzheimer's agents: DFT, molecular docking, enzyme inhibition and pharmacokinetic studies.
RSC Med Chem 13: 1644-1656 (2022)
Federal University of Santa Catarina
Revisiting a challenging p53 binding site: a diversity-optimized HEFLib reveals diverse binding modes in T-p53C-Y220C.
RSC Med Chem 13: 1575-1586 (2022)
Universit�T T�Bingene
Structure-activity relationship study of PROTACs against hematopoietic prostaglandin D
RSC Med Chem 13: 1495-1503 (2022)
National Institute of Health Sciences
Recent advances toward the development of Hsp90 C-terminal inhibitors.
Bioorg Med Chem Lett 80: (2023)
University of Notre Dame
Novel imidazo[1,5-a]quinoxaline derivatives: SAR, selectivity and modeling challenges en route to the identification of an α5-GABAA receptor NAM.
Bioorg Med Chem Lett 80: (2023)
Gedeon Richter
Discovery of potent 1,1-diarylthiogalactoside glycomimetic inhibitors of Pseudomonas aeruginosa LecA with antibiofilm properties.
Eur J Med Chem 247: (2023)
University Paris-Saclay
Natural product evodiamine-inspired medicinal chemistry: Anticancer activity, structural optimization and structure-activity relationship.
Eur J Med Chem 247: (2023)
University of South China
Novel pyridine-containing histone deacetylase inhibitors strongly arrest proliferation, induce apoptosis and modulate miRNAs in cancer cells.
Eur J Med Chem 247: (2023)
Sapienza University of Rome
Structure-based lead optimization of peptide-based vinyl methyl ketones as SARS-CoV-2 main protease inhibitors.
Eur J Med Chem 247: (2023)
University of Messina
Tetracyclic Steroids Bearing a Bicyclo[4.4.1] Ring System as Potent Antiosteoporosis Agents from the Deep-Sea-Derived Fungus
J Nat Prod 86: 157-165 (2023)
Third Institute of Oceanography
A high-throughput effector screen identifies a novel small molecule scaffold for inhibition of ten-eleven translocation dioxygenase 2.
RSC Med Chem 13: 1540-1548 (2022)
Tu Dortmund University
Pyrazolone derivatives as potent and selective small-molecule SIRT5 inhibitors.
Eur J Med Chem 247: (2023)
University of Michigan
Multitargeting approaches to cognitive impairment: Synthesis of aryl-alkylpiperazines and assessment at cholinesterases, histamine H
Bioorg Med Chem 78: (2023)
Universidade Federal De Sao Paulo
Harnessing polyhydroxylated pyrrolidines as a stabilizer of acid alpha-glucosidase (GAA) to enhance the efficacy of enzyme replacement therapy in Pompe disease.
Bioorg Med Chem 78: (2023)
National Yang Ming Chiao Tung University
Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
Bioorg Med Chem 78: (2023)
Institute of Mit and Harvard
Development of
J Med Chem 66: 235-250 (2023)
University Degli Studi Di Bari Aldo Moro
Discovery of Macrocycle-Based HPK1 Inhibitors for T-Cell-Based Immunotherapy.
J Med Chem 66: 611-626 (2023)
Central China Normal University
Chemical Blockage of the Mitochondrial Rhomboid Protease PARL by Novel Ketoamide Inhibitors Reveals Its Role in PINK1/Parkin-Dependent Mitophagy.
J Med Chem 66: 251-265 (2023)
Institute of Organic Chemistry and Biochemistry of The Czech Academy of Science
Discovery of Spiro[pyrrolidine-3,3'-oxindole] LXRβ Agonists for the Treatment of Osteoporosis.
J Med Chem 66: 752-765 (2023)
Sun Yat-Sen University
Discovery of structural diverse reversible BTK inhibitors utilized to develop a novel in vivo CD69 and CD86 PK/PD mouse model.
Bioorg Med Chem Lett 80: (2023)
Amgen
Discovery of the First Lactate Dehydrogenase Proteolysis Targeting Chimera Degrader for the Treatment of Pancreatic Cancer.
J Med Chem 66: 596-610 (2023)
Icahn School of Medicine At Mount Sinai
Structural Alterations of the "Address" Moiety of NAN Leading to the Discovery of a Novel Opioid Receptor Modulator with Reduced hERG Toxicity.
J Med Chem 66: 577-595 (2023)
Virginia Commonwealth University
Small Molecule Inhibitors of Protein Kinase D: Early Development, Current Approaches, and Future Directions.
J Med Chem 66: 122-139 (2023)
University of Pittsburgh
Structural and Functional Landscape of FAD-Dependent Histone Lysine Demethylases for New Drug Discovery.
J Med Chem 66: 71-94 (2023)
Zhengzhou University
Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors.
J Med Chem 66: 149-169 (2023)
Revolution Medicines
Rational Design of a New RXR Agonist Scaffold Enabling Single-Subtype Preference for RXRα, RXRβ, and RXRγ.
J Med Chem 66: 333-344 (2023)
Goethe University Frankfurt
Discovery of a Series of Potent, Selective, and Orally Bioavailable Nucleoside Inhibitors of CD73 That Demonstrates
J Med Chem 66: 345-370 (2023)
Calithera Biosciences
Alkaloids and Coumarins with Adiponectin-Secretion-Promoting Activities from the Leaves of
J Nat Prod 86: 138-148 (2023)
Seoul National University
Discovery of cysteine-targeting covalent histone methyltransferase inhibitors.
Eur J Med Chem 246: (2023)
Nanjing Medical University
Persistent challenges in the development of an mGlu
Bioorg Med Chem Lett 80: (2023)
Vanderbilt University
Discovery of tetrahydrofuranyl spirooxindole-based SMYD3 inhibitors against gastric cancer via inducing lethal autophagy.
Eur J Med Chem 246: (2023)
Chengdu University of Traditional Chinese Medicine
Subnanomolar Affinity and Selective Antagonism at α7 Nicotinic Receptor by Combined Modifications of 2-Triethylammonium Ethyl Ether of 4-Stilbenol (MG624).
J Med Chem 66: 306-332 (2023)
University of Milan
Design, synthesis, and biological evaluation of novel glutaminase 1 allosteric inhibitors with an alkane chain tail group.
Eur J Med Chem 246: (2023)
China Pharmaceutical University
Discovery of Clinical Candidate AZD0095, a Selective Inhibitor of Monocarboxylate Transporter 4 (MCT4) for Oncology.
J Med Chem 66: 384-397 (2023)
Astrazeneca
Identification of N- and C-3-Modified Laudanosoline Derivatives as Novel Influenza PA
J Med Chem 66: 188-219 (2023)
South China Agricultural University
Design of Cytochrome P450 1B1 Inhibitors
J Med Chem 66: 398-412 (2023)
University of Kentucky
Structure-Activity Relationship Study of Tertiary Alcohol Hsp90α-Selective Inhibitors with Novel Binding Mode.
ACS Med Chem Lett 13: 1870-1878 (2022)
The University of Notre Dame
Pyrazolidine Carboxamide Analogs as Selective Agonists of the Cannabinoid 2 Receptor.
ACS Med Chem Lett 13: 1837-1838 (2022)
Arrival Discovery
Effects of 6-Aminonicotinic Acid Esters on the Reprogrammed Epigenetic State of Distant Metastatic Pancreatic Carcinoma.
ACS Med Chem Lett 13: 1892-1897 (2022)
Johns Hopkins University School of Medicine
Identification of a Target Site for Covalent Inhibition of Protein Phosphohistidine Phosphatase 1.
ACS Med Chem Lett 13: 1911-1915 (2022)
Ulsan National Institute of Science and Technology (UNIST)
Optimization of First-in-Class Dual-Acting FFAR1/FFAR4 Allosteric Modulators with Novel Mode of Action.
ACS Med Chem Lett 13: 1839-1847 (2022)
University of Copenhagen
Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448).
ACS Med Chem Lett 13: 1856-1863 (2022)
The State University of New York
Fragment-Sized Thiazoles in Fragment-Based Drug Discovery Campaigns: Friend or Foe?
ACS Med Chem Lett 13: 1905-1910 (2022)
University of Ljubljana
Exploring the Effect of Halogenation in a Series of Potent and Selective A
J Med Chem 66: 890-912 (2023)
University of Santiago de Compostela
Design, synthesis, biological evaluation and crystal structure determination of dual modulators of carbonic anhydrases and estrogen receptors.
Eur J Med Chem 246: (2023)
University of Modena and Reggio Emilia
MSC-1186, a Highly Selective Pan-SRPK Inhibitor Based on an Exceptionally Decorated Benzimidazole-Pyrimidine Core.
J Med Chem 66: 837-854 (2023)
Goethe University Frankfurt
The Identification of Potent, Selective, and Brain Penetrant PI5P4Kγ Inhibitors as In Vivo-Ready Tool Molecules.
J Med Chem 66: 804-821 (2023)
University of Cambridge
Discovery of Novel Acridane-Based Tubulin Polymerization Inhibitors with Anticancer and Potential Immunomodulatory Effects.
J Med Chem 66: 627-640 (2023)
Gannan Medical University
Discovery and Development of a Selective Inhibitor of the ER Resident Chaperone Grp78.
J Med Chem 66: 677-694 (2023)
University of Arizona
Structure-Based Drug Design and Synthesis of Novel
J Med Chem 65: 16451-16480 (2022)
Shenyang Pharmaceutical University
Identification of TUL01101: A Novel Potent and Selective JAK1 Inhibitor for the Treatment of Rheumatoid Arthritis.
J Med Chem 65: 16716-16740 (2022)
Zhuhai United Laboratories
Discovery of Novel Orally Bioavailable Triazoles with Potent and Broad-Spectrum Antifungal Activity In Vitro and In Vivo.
J Med Chem 65: 16665-16678 (2022)
Tongji University
Multi-therapies Based on PARP Inhibition: Potential Therapeutic Approaches for Cancer Treatment.
J Med Chem 65: 16099-16127 (2022)
Shandong First Medical University and Shandong Academy of Medical Sciences
Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site.
J Med Chem 65: 16372-16391 (2022)
Peking Union Medical College
Design, synthesis and biological evaluation of novel 3,4-dihydro-2H-[1,4]oxazino [2,3-f]quinazolin derivatives as EGFR-TKIs.
Bioorg Med Chem Lett 80: (2023)
Guangxi Minzu University
Design, synthesis, and pharmacological evaluations of pyrrolo[1,2-a]quinoxaline-based derivatives as potent and selective sirt6 activators.
Eur J Med Chem 246: (2023)
University of Texas Medical Branch
Novel 3-Trifluoromethyl-1,2,4-oxadiazole Analogues of Astemizole with Multi-stage Antiplasmodium Activity and
J Med Chem 65: 16695-16715 (2022)
University of Cape Town
Structure, Function, and Inhibitors of the Mitochondrial Chaperone TRAP1.
J Med Chem 65: 16155-16172 (2022)
Ewha Womans University
Structure-Based Design of a Dual-Targeted Covalent Inhibitor Against Papain-like and Main Proteases of SARS-CoV-2.
J Med Chem 65: 16252-16267 (2022)
China Pharmaceutical University
Targeting the PI3K/AKT/mTOR Signaling Pathway in the Treatment of Human Diseases: Current Status, Trends, and Solutions.
J Med Chem 65: 16033-16061 (2022)
South China University of Technology
A concise review on marine bromopyrrole alkaloids as anticancer agents.
Bioorg Med Chem Lett 80: (2023)
University of Kwazulu-Natal (Westville)
Combining pharmacophore models derived from DNA-encoded chemical libraries with structure-based exploration to predict Tankyrase 1 inhibitors.
Eur J Med Chem 246: (2023)
University of Utah
New bioisosteric sulphur-containing choline kinase inhibitors with a tracked mode of action.
Eur J Med Chem 246: (2023)
University of Granada
The Emerging Landscape of Small-Molecule Therapeutics for the Treatment of Huntington's Disease.
J Med Chem 65: 15993-16032 (2022)
Aligarh Muslim University
Synthesis, Characterization, and Application of Muscarinergic M
J Med Chem 65: 16494-16509 (2022)
Friedrich-Alexander-Universitat Erlangen-Nurnberg
Structure based design and evaluation of benzoheterocycle derivatives as potential dual HIV-1 protease and reverse transcriptase inhibitors.
Eur J Med Chem 246: (2023)
Peking Union Medical College
Synthesis and biological evaluation of N-(benzene sulfonyl)acetamide derivatives as anti-inflammatory and analgesic agents with COX-2/5-LOX/TRPV1 multifunctional inhibitory activity.
Bioorg Med Chem Lett 80: (2023)
Anhui University of Chinese Medicine
Discovery of 2-Amino-7-sulfonyl-7
J Med Chem 65: 16570-16588 (2022)
China Pharmaceutical University
Design and Optimization of 1
J Med Chem 65: 16829-16859 (2022)
St. Jude Children'S Research Hospital
Synthesis of novel glutarimide ligands for the E3 ligase substrate receptor Cereblon (CRBN): Investigation of their binding mode and antiproliferative effects against myeloma cell lines.
Eur J Med Chem 246: (2023)
Saint Petersburg State University
Discovery and Optimization of Potent, Selective, and Brain-Penetrant 1-Heteroaryl-1
J Med Chem 65: 16801-16817 (2022)
Merck
Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivatives as Covalent SARS-CoV-2 Main Protease Inhibitors.
J Med Chem 65: 16902-16917 (2022)
Shandong University
BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
J Med Chem 65: 16420-16431 (2022)
Bayer
Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates.
J Med Chem 65: 16234-16251 (2022)
Merck
Discovery of Pan-peroxisome Proliferator-Activated Receptor Modulators from an Endolichenic Fungus,
J Nat Prod 85: 2804-2816 (2022)
Seoul National University
Tricyclic SpiroLactams Kill Mycobacteria In Vitro and In Vivo by Inhibiting Type II NADH Dehydrogenases.
J Med Chem 65: 16651-16664 (2022)
Cnrs
Solid-Phase Synthesis of Cereblon-Recruiting Selective Histone Deacetylase 6 Degraders (HDAC6 PROTACs) with Antileukemic Activity.
J Med Chem 65: 16860-16878 (2022)
Leipzig University
Targeting Sterol
J Med Chem 65: 16062-16098 (2022)
National Institute On Alcohol Abuse and Alcoholism
Structure-Based Design of Tropane Derivatives as a Novel Series of CCR5 Antagonists with Broad-Spectrum Anti-HIV-1 Activities and Improved Oral Bioavailability.
J Med Chem 65: 16526-16540 (2022)
Shanghai Institute of Materia Medica
Chlorinated Naringenin Analogues as Potential Inhibitors of Transthyretin Amyloidogenesis.
J Med Chem 65: 16218-16233 (2022)
University of Toyama
Discovery of Novel
J Med Chem 65: 16774-16800 (2022)
China Pharmaceutical University
Design, synthesis and anti-ovarian cancer activities of thieno[2,3-d]pyrimidine based chimeric BRD4 inhibitor/nitric oxide-donator.
Eur J Med Chem 246: (2023)
Sichuan University
Design and synthesis of new adamantyl derivatives as promising antiproliferative agents.
Eur J Med Chem 246: (2023)
University of Sharjah
Discovery of Potent and Selective Dual Leucine Zipper Kinase/Leucine Zipper-Bearing Kinase Inhibitors with Neuroprotective Properties in In Vitro and In Vivo Models of Amyotrophic Lateral Sclerosis.
J Med Chem 65: 16290-16312 (2022)
Denali Therapeutics
Resveratrol derivatives: Synthesis and their biological activities.
Eur J Med Chem 246: (2023)
Universitat De Barcelona
Exploration of 1,2,3-triazole linked benzenesulfonamide derivatives as isoform selective inhibitors of human carbonic anhydrase.
Bioorg Med Chem 77: (2023)
Sakarya University
Discovery of novel 7,7-dimethyl-6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidines as ATR inhibitors based on structure-based drug design.
Eur J Med Chem 246: (2023)
Shenyang Pharmaceutical University
Resorcinol-based hemiindigoid derivatives as human tyrosinase inhibitors and melanogenesis suppressors in human melanoma cells.
Eur J Med Chem 246: (2023)
University Grenoble Alpes
Novel slow-binding reversible acetylcholinesterase inhibitors based on uracil moieties for possible treatment of myasthenia gravis and protection from organophosphate poisoning.
Eur J Med Chem 246: (2023)
Frc Kazan Scientific Center of Ras
Discovery of orally active 1,4,5,6,8-pentaazaacenaphthylens as novel, selective, and potent covalent BTK inhibitors for the treatment of rheumatoid arthritis.
Eur J Med Chem 246: (2023)
China Pharmaceutical University
Recent advances in PI3K/PKB/mTOR inhibitors as new anticancer agents.
Eur J Med Chem 246: (2023)
University of Calabria
Development of potent and selective FAAH inhibitors with improved drug-like properties as potential tools to treat neuroinflammatory conditions.
Eur J Med Chem 246: (2023)
Universit£
Structure-activity relationship study of amidobenzimidazole derivatives as stimulator of interferon genes (STING) agonists.
Eur J Med Chem 246: (2023)
Peking Union Medical College
Discovery of novel N-acylpyrazoles as potent and selective thrombin inhibitors.
Eur J Med Chem 246: (2023)
Verseon
Design, synthesis, and evaluation of tricyclic compounds containing phenyl-tetrazole as XOR inhibitors.
Eur J Med Chem 246: (2023)
South China University of Technology
Pyrimidine derivatives with antitubercular activity.
Eur J Med Chem 246: (2023)
Charles University
Design, synthesis and evaluation of N3-substituted quinazolinone derivatives as potential Bloom's Syndrome protein (BLM) helicase inhibitor for sensitization treatment of colorectal cancer.
Eur J Med Chem 246: (2023)
Sun Yat-Sen University
The Highly Potent AhR Agonist Picoberin Modulates Hh-Dependent Osteoblast Differentiation.
J Med Chem 65: 16268-16289 (2022)
Max Planck Institute of Molecular Physiology
A Comprehensive Overview of Small-Molecule Androgen Receptor Degraders: Recent Progress and Future Perspectives.
J Med Chem 65: 16128-16154 (2022)
China Pharmaceutical University
Design, synthesis, and bioevaluation of imidazo [1,2-a] pyrazine derivatives as tubulin polymerization inhibitors with potent anticancer activities.
Bioorg Med Chem 76: (2022)
Southern Medical University
Novel rhodanine based inhibitors of aldose reductase of non-acidic nature with p-hydroxybenzylidene functional group.
Eur J Med Chem 246: (2023)
Charles University
Rational design of novel nucleoside analogues reveals potent antiviral agents for EV71.
Eur J Med Chem 246: (2023)
Swansea University
Synthesis and structure-activity relationship studies of original cyclic diadenosine derivatives as nanomolar inhibitors of NAD kinase from pathogenic bacteria.
Eur J Med Chem 246: (2023)
University Paris Cite
Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.
J Med Chem 65: 16589-16621 (2022)
Genentech
Discovery of Orally Bioavailable
J Med Chem 65: 16622-16639 (2022)
China Pharmaceutical University
Computational design, synthesis and biological evaluation of PDE5 inhibitors based on N
Bioorg Med Chem 76: (2022)
King Mongkut'S Institute of Technology
Optimization of 1,2,4-Triazole-3-thiones toward Broad-Spectrum Metallo-β-lactamase Inhibitors Showing Potent Synergistic Activity on VIM- and NDM-1-Producing Clinical Isolates.
J Med Chem 65: 16392-16419 (2022)
Univ Montpellier
Design and Synthesis of Fibroblast Growth Factor Receptor (FGFR) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Cancer.
J Med Chem 65: 16541-16569 (2022)
Sichuan University
Development of Alkylated Hydrazides as Highly Potent and Selective Class I Histone Deacetylase Inhibitors with T cell Modulatory Properties.
J Med Chem 65: 16313-16337 (2022)
Martin-Luther University of Halle-Wittenberg
Discovery and Optimization of Potent and Orally Available CTP Synthetase Inhibitors for Use in Treatment of Diseases Driven by Aberrant Immune Cell Proliferation.
J Med Chem 65: 16640-16650 (2022)
Sygnature Discovery
Recent Update on the Development of PCSK9 Inhibitors for Hypercholesterolemia Treatment.
J Med Chem 65: 15513-15539 (2022)
Aligarh Muslim University
Briarane-type diterpenoids, the inhibitors of osteoclast formation by interrupting Keap1-Nrf2 interaction and activating Nrf2 pathway.
Eur J Med Chem 246: (2023)
Peking University
Disubstituted pyrimidine-5-carboxamide derivatives as novel HIV-1 NNRTIs: Crystallographic overlay-based molecular design, synthesis, and biological evaluation.
Eur J Med Chem 246: (2023)
Shandong University
Making Protein Degradation Visible: Discovery of Theranostic PROTACs for Detecting and Degrading NAMPT.
J Med Chem 65: 15725-15737 (2022)
Second Military Medical University (Navy Medical University)
Structure-guided design of novel HEPT analogs with enhanced potency and safety: From Isopropyl-HEPTs to Cyclopropyl-HEPTs.
Eur J Med Chem 246: (2023)
Zhejiang University
B-cell Lymphoma 6 Inhibitors: Current Advances and Prospects of Drug Development for Diffuse Large B-cell Lymphomas.
J Med Chem 65: 15559-15583 (2022)
East China Normal University
What We Have Gained from Ibogaine: α3β4 Nicotinic Acetylcholine Receptor Inhibitors as Treatments for Substance Use Disorders.
J Med Chem 66: 107-121 (2023)
University of Illinois At Chicago
Synthesis of full-length homodimer αD-VxXXB that targets human α7 nicotinic acetylcholine receptors.
RSC Med Chem 13: 1410-1419 (2022)
The University of Queensland
Efficient selective targeting of
RSC Med Chem 13: 1322-1340 (2022)
University of Sharjah
Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies.
RSC Med Chem 13: 1300-1321 (2022)
Tianjin University
Novel 4-aminoquinolines: Synthesis, inhibition of the Mycobacterium tuberculosis enoyl-acyl carrier protein reductase, antitubercular activity, SAR, and preclinical evaluation.
Eur J Med Chem 245: (2023)
Pontifical Catholic University of Rio Grande Do Sul
Design and synthesis of dual cathepsin L and S inhibitors and antimetastatic activity evaluation in pancreatic cancer cells.
Bioorg Med Chem Lett 80: (2023)
Shenyang Pharmaceutical University
A fragment-based approach leading to the discovery of inhibitors of CK2α with a novel mechanism of action.
RSC Med Chem 13: 1420-1426 (2022)
University of Cambridge
Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non-small cell lung cancer.
Bioorg Med Chem Lett 80: (2023)
Ariad Pharmaceuticals
Design, development and evaluation of a prodrug-type TrkA-selective inhibitor with antinociceptive effects in vivo.
Eur J Med Chem 245: (2023)
Fudan University
Recent advances of novel fourth generation EGFR inhibitors in overcoming C797S mutation of lung cancer therapy.
NA
Hangzhou Normal University
Development and Utility of a PAK1-Selective Degrader.
J Med Chem 65: 15627-15641 (2022)
Fox Chase Cancer Center
Identification of a Novel Potent CYP4Z1 Inhibitor Attenuating the Stemness of Breast Cancer Cells through Lead Optimization.
J Med Chem 65: 15749-15769 (2022)
China Pharmaceutical University
Design, synthesis and biological evaluation of cajanonic acid A analogues as potent PPAR γ antagonists.
Bioorg Med Chem Lett 80: (2023)
Guizhou Medical University
Lead Optimization and Avoidance of Metabolic-perturbing Motif Developing Novel Diarylpyrimidines as Potent HIV-1 NNRTIs.
J Med Chem 65: 15608-15626 (2022)
Shandong University
Switch type I to type II TRK inhibitors for combating clinical resistance induced by xDFG mutation for cancer therapy.
Eur J Med Chem 245: (2023)
Jinan University
Pose, duplicate, then elaborate: Steps towards increased affinity for inhibitors targeting the specificity surface of the Pim-1 kinase.
Eur J Med Chem 245: (2023)
Philipps-Universit£T Marburg
Identification and Characterization of a Novel Indoleamine 2,3-Dioxygenase 1 Protein Degrader for Glioblastoma.
J Med Chem 65: 15642-15662 (2022)
Northwestern University Feinberg School of Medicine
Identification of novel benzimidazole derivatives as highly potent AMPK activators with anti-diabetic profiles.
Bioorg Med Chem Lett 79: (2023)
Shionogi
The discovery of (1R, 3R)-1-(3-chloro-5-fluorophenyl)-3-(hydroxymethyl)-1,2,3,4-tetrahydroisoquinoline-6-carbonitrile, a potent and selective agonist of human transient receptor potential cation channel subfamily m member 5 (TRPM5) and evaluation of as a potential gastrointestinal prokinetic agent.
Bioorg Med Chem 76: (2022)
Turning Point Therapeutics
Identification of potent and selective inhibitors of PKR via virtual screening and traditional design.
Bioorg Med Chem Lett 79: (2023)
Abbvie Bioresearch Center
Acyloxymethyl and alkoxycarbonyloxymethyl prodrugs of a fosmidomycin surrogate as antimalarial and antibacterial agents.
Eur J Med Chem 245: (2023)
Ghent University
Development of novel hydrazidoarylaminopyrimidine-based BTK/FLT3 dual inhibitors with potent in vivo anti-hematological malignancies effects.
Eur J Med Chem 245: (2023)
Nantong University
Histone deacetylases (HDACs) as the promising immunotherapeutic targets for hematologic cancer treatment.
Eur J Med Chem 245: (2023)
Zhengzhou University
Discovery and Optimization of
J Med Chem 65: 15710-15724 (2022)
Zhejiang University
Selective Inhibition of PTP1B by New Anthraquinone Glycosides from
J Nat Prod 85: 2836-2844 (2022)
Binzhou Medical University
JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS
J Med Chem 65: 16173-16203 (2022)
Novartis Institutes For Biomedical Research
Novel α7 nicotinic acetylcholine receptor modulators as potential antitussive agents.
Bioorg Med Chem Lett 80: (2023)
Philip Morris International
New cycloalkyl[b]thiophenylnicotinamide-based α-glucosidase inhibitors as promising anti-diabetic agents: Synthesis, in silico study, in vitro and in vivo evaluations.
Bioorg Med Chem Lett 79: (2023)
University of Jinan
Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells.
Bioorg Med Chem 75: (2022)
The Affiliated Hospital of Southwest Medical University
Antiproliferative, antiangiogenic and apoptotic effect of new hybrids of quinazoline-4(3H)-ones and sulfachloropyridazine.
Eur J Med Chem 245: (2023)
National Center for Radiation Research and Technology (NCRRT)
Research progress and challenges of TRPV1 channel modulators as a prospective therapy for diabetic neuropathic pain.
Eur J Med Chem 245: (2023)
The First Affiliated Hospital of Zhengzhou University
Identification of novel Pyrrolo[2,3-d]Pyrimidine-based KRAS G12C inhibitors with anticancer effects.
Eur J Med Chem 245: (2023)
Sun Yat-Sen University
Novel 1,4,5,6-tetrahydrocyclopenta[d]imidazole-5-carboxamide-based JNK3 inhibitors: Design, synthesis, molecular docking, and therapeutic potential in neurodegenerative diseases.
Eur J Med Chem 245: (2023)
Hanyang University
Targeting Gatekeeper Mutations for Kinase Drug Discovery.
J Med Chem 65: 15540-15558 (2022)
Jinan University
Discovery of a Series of 5-Amide-1
J Med Chem 65: 15967-15990 (2022)
China Pharmaceutical University
A New Naphthopyran Derivative Combines
ACS Med Chem Lett 13: 1783-1790 (2022)
University of Bayreuth
Covalent Modification of the JH2 Domain of Janus Kinase 2.
ACS Med Chem Lett 13: 1819-1826 (2022)
Yale University
Identification of Inhibitors of the
ACS Med Chem Lett 13: 1715-1722 (2022)
Imperial College London
Recent Discovery of PARP7 Inhibitors as Anticancer Agents.
ACS Med Chem Lett 13: 1688-1690 (2022)
Usona Institute
Discovery of Selective Inhibitors of Na
ACS Med Chem Lett 13: 1763-1768 (2022)
Siteone Therapeutics
Inhibition of β-Amyloid Aggregation in Alzheimer's Disease: The Key Role of (Pro)electrophilic Warheads.
ACS Med Chem Lett 13: 1812-1818 (2022)
Alma Mater Studiorum - University of Bologna
(-)-Epigallocatechin Gallate is a Noncompetitive Inhibitor of NAD Kinase.
ACS Med Chem Lett 13: 1699-1706 (2022)
Hangzhou Institute For Advanced Study
Discovery of κ Opioid Receptor (KOR)-Selective d-Tetrapeptides with Improved
ACS Med Chem Lett 13: 1707-1714 (2022)
D'Annunzio University of Chieti���Pescara
Novel TYK2 Inhibitors with an
ACS Med Chem Lett 13: 1730-1738 (2022)
Nanjing University of Science and Technology
Optimization of Pyrimidine Compounds as Potent JAK1 Inhibitors and the Discovery of R507 as a Clinical Candidate.
ACS Med Chem Lett 13: 1805-1811 (2022)
Rigel Pharmaceuticals
The Invention of WM382, a Highly Potent PMIX/X Dual Inhibitor toward the Treatment of Malaria.
ACS Med Chem Lett 13: 1745-1754 (2022)
Merck
Discovery of Novel
J Med Chem 65: 15770-15788 (2022)
Shenyang Pharmaceutical University
Design and Structural Optimization of Orally Bioavailable SOS1 Inhibitors for the Treatment of KRAS-Driven Carcinoma.
J Med Chem 65: 15856-15877 (2022)
Wuhan University of Science and Technology
Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.
J Med Chem 65: 15679-15697 (2022)
Goethe University Frankfurt
Engineering the Cyclization Loop of MCoTI-II Generates Targeted Cyclotides that Potently Inhibit Factor XIIa.
J Med Chem 65: 15698-15709 (2022)
The University of Queensland
Discovery of PPARγ and glucocorticoid receptor dual agonists to promote the adiponectin and leptin biosynthesis in human bone marrow mesenchymal stem cells.
Eur J Med Chem 245: (2023)
Seoul National University
Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432.
J Med Chem 65: 15174-15207 (2022)
Gsk
Selective TASK-1 Inhibitor with a Defined Structure-Activity Relationship Reduces Cancer Cell Proliferation and Viability.
J Med Chem 65: 15014-15027 (2022)
Centro De Estudios En Alimentos Procesados-Ceap
Development of Macrocyclic PRMT5-Adaptor Protein Interaction Inhibitors.
J Med Chem 65: 15300-15311 (2022)
Max Planck Institute of Molecular Physiology
Design, synthesis, and biological evaluation of novel quinoline derivatives as small molecule mutant EGFR inhibitors targeting resistance in NSCLC: In vitro screening and ADME predictions.
Eur J Med Chem 245: (2023)
Radhabai Kale Mahila Mahavidyalaya
Structural optimization and biological evaluation of 1-adamantylcarbonyl-4-phenylpiperazine derivatives as FXR agonists for NAFLD.
Eur J Med Chem 245: (2023)
Chinese Academy of Medical Sciences&Peking Union Medical College
Natural quinazolinones: From a treasure house to promising anticancer leads.
Eur J Med Chem 245: (2023)
Yale University
Discovery of novel hydroxyamidine based indoleamine 2,3-dioxygenase 1 (IDO1) and thioredoxin reductase 1 (TrxR1) dual inhibitors.
Eur J Med Chem 245: (2023)
Wannan Medical College
Design, synthesis and biological evaluation of a new class of 7H-pyrrolo[2,3-d]pyrimidine derivatives as Mps1 inhibitors for the treatment of breast cancer.
Eur J Med Chem 245: (2023)
Sichuan University
Lead identification of novel tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid derivative as a potent heparanase-1 inhibitor.
Bioorg Med Chem Lett 79: (2023)
Taisho Pharmaceutical Co.
Discovery of oxazoline enhancers of cellular progranulin release.
Bioorg Med Chem Lett 80: (2023)
Arkuda Therapeutics
Structure-Activity Studies of 1
J Med Chem 65: 15238-15262 (2022)
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of novel N-(1-benzyl-1H-imidazol-2-yl)amide derivatives as melanocortin 1 receptor agonists.
Bioorg Med Chem Lett 78: (2022)
Mitsubishi Tanabe Pharma
Mapping Ligand Interactions of Bromodomains BRD4 and ATAD2 with FragLites and PepLites─Halogenated Probes of Druglike and Peptide-like Molecular Interactions.
J Med Chem 65: 15416-15432 (2022)
Newcastle University Centre For Cancer
Discovery of 3-Aminopyrazole Derivatives as New Potent and Orally Bioavailable AXL Inhibitors.
J Med Chem 65: 15374-15390 (2022)
Jinan University
Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.
J Med Chem 65: 15433-15442 (2022)
Prelude Therapeutics
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.
J Med Chem 65: 15227-15237 (2022)
University of Science and Technology of China
Discovery of D6808, a Highly Selective and Potent Macrocyclic c-Met Inhibitor for Gastric Cancer Harboring
J Med Chem 65: 15140-15164 (2022)
Jinan University
Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia.
J Med Chem 65: 15457-15472 (2022)
University of Bonn
Exploration and Biological Evaluation of Bispecific Peptides Derived from Anti-HER2 Antibodies and Peptide-Camptothecin Conjugates for HER2-Positive Breast Cancer.
J Med Chem 65: 15123-15139 (2022)
China Pharmaceutical University
Discovery, Optimization, and Evaluation of Selective CDK4/6 Inhibitors for the Treatment of Breast Cancer.
J Med Chem 65: 15102-15122 (2022)
China Pharmaceutical University
Design, synthesis, and biological studies of dual URAT1 inhibitor and FXR agonist based on benzbromarone.
Bioorg Med Chem 75: (2022)
Guangdong Pharmaceutical University
Discovery and development of palmatine analogues as anti-NASH agents by activating farnesoid X receptor (FXR).
Eur J Med Chem 245: (2023)
Chinese Academy of Medical Sciences & Peking Union Medical College
Small-Molecule Receptor-Interacting Protein 1 (RIP1) Inhibitors as Therapeutic Agents for Multifaceted Diseases: Current Medicinal Chemistry Insights and Emerging Opportunities.
J Med Chem 65: 14971-14999 (2022)
West China Hospital
Phenotypic Discovery of Triazolo[1,5-
J Med Chem 65: 15263-15281 (2022)
Technical University Dortmund
Design, Synthesis, and Pharmacological Evaluation of Second-Generation Soluble Adenylyl Cyclase (sAC, ADCY10) Inhibitors with Slow Dissociation Rates.
J Med Chem 65: 15208-15226 (2022)
Tri-Institutional Institutional Therapeutics Discovery Institute
Exploring the NCS-382 Scaffold for CaMKIIα Modulation: Synthesis, Biochemical Pharmacology, and Biophysical Characterization of Ph-HTBA as a Novel High-Affinity Brain-Penetrant Stabilizer of the CaMKIIα Hub Domain.
J Med Chem 65: 15066-15084 (2022)
University of Copenhagen
Synthesis and in vitro biological evaluation of 3-ethyl-1,5-naphthyridin-2(1H)-one derivatives as potent PARP-1 selective inhibitors and PARP-1 DNA trappers.
Bioorg Med Chem Lett 78: (2022)
China Pharmaceutical University
From rational design to serendipity: Discovery of novel thiosemicarbazones as potent trypanocidal compounds.
Eur J Med Chem 244: (2022)
Federal University of Minas Gerais
Discovery of novel imidazole chemotypes as isoform-selective JNK3 inhibitors for the treatment of Alzheimer's disease.
Eur J Med Chem 245: (2023)
Hanyang University
Discovery of a structurally novel, potent, and once-weekly free fatty acid receptor 1 agonist for the treatment of diabetes.
Eur J Med Chem 245: (2023)
Guangdong Pharmaceutical University
Photoredox-based late-stage functionalization in SAR study for in vivo potent glucosylceramide synthase inhibitor.
Bioorg Med Chem Lett 77: (2022)
Takeda Pharmaceutical
Novel ginsenoside derivatives induce apoptosis in HepG-2 cells via the MDM2-p53 signaling pathway.
Bioorg Med Chem Lett 78: (2022)
Shenyang Pharmaceutical University
CSF1R inhibitors are emerging immunotherapeutic drugs for cancer treatment.
NA
Shenyang Pharmaceutical University
Covalently Conjugated NOD2/TLR7 Agonists Are Potent and Versatile Immune Potentiators.
J Med Chem 65: 15085-15101 (2022)
University of Ljubljana
Synthesis and antineoplastic activity of ethylene glycol phenyl aminoethyl ether derivatives as FOXM1 inhibitors.
Eur J Med Chem 244: (2022)
Peking Union Medical College
Synthesis, evaluation and mechanism exploration of 2-(N-(3-nitrophenyl)-N-phenylsulfonyl)aminoacetohydroxamic acids as novel urease inhibitors.
Bioorg Med Chem Lett 78: (2022)
National Demonstration Center For Experimental Chemistry Education
Design and synthesis of boron-containing ALK inhibitor with favorable in vivo efficacy.
Bioorg Med Chem 75: (2022)
Nanjing University
Identification of 1,2,3-triazolium salt-based inhibitors of Leishmania infantum trypanothione disulfide reductase with enhanced antileishmanial potency in cellulo and increased selectivity.
Eur J Med Chem 244: (2022)
Universidad De Alcal£
Design, synthesis and anticancer evaluation of selective 2,4-disubstituted pyrimidine CDK9 inhibitors.
Eur J Med Chem 244: (2022)
Southeast University
Current approaches and strategies to identify Hedgehog signaling pathway inhibitors for cancer therapy.
Eur J Med Chem 244: (2022)
Peking Union Medical College
Rational design of the zonulin inhibitor AT1001 derivatives as potential anti SARS-CoV-2.
Eur J Med Chem 244: (2022)
European Biomedical Research Institute of Salerno (Ebris)
C-6 fluorinated casuarines as highly potent and selective amyloglucosidase inhibitors: Synthesis and structure-activity relationship study.
Eur J Med Chem 244: (2022)
Beijing National Laboratory For Molecular Sciences
Easy access to α-ketoamides as SARS-CoV-2 and MERS M
Eur J Med Chem 244: (2022)
University of Naples Federico Ii
Targefrin: A Potent Agent Targeting the Ligand Binding Domain of EphA2.
J Med Chem 65: 15443-15456 (2022)
University of California Riverside
A 1,2,3-Triazole Derivative of Quinazoline Exhibits Antitumor Activity by Tethering RNF168 to SQSTM1/P62.
J Med Chem 65: 15028-15047 (2022)
Shenzhen University School of Medicine
Targeting osteoarthritis-associated galectins and an induced effector class by a ditopic bifunctional reagent: Impact of its glycan part on binding measured in the tissue context.
Bioorg Med Chem 75: (2022)
Ludwig-Maximilians-University Munich
Semisynthesis, biological activities, and mechanism studies of Mannich base analogues of magnolol/honokiol as potential α-glucosidase inhibitors.
Bioorg Med Chem 75: (2022)
Zhengzhou University
Enhancing the Safety and Efficacy of PSMA-Based Small-Molecule Drug Conjugates by Linker Stabilization and Conjugation to Transthyretin Binding Ligand.
J Med Chem 65: 15473-15486 (2022)
University of The Pacific
Structure-based discovery of potent inhibitors of Axl: design, synthesis, and biological evaluation.
RSC Med Chem 13: 1246-1264 (2022)
Hunan Normal University
Insights into the medicinal chemistry of heterocycles integrated with a pyrazolo[1,5-
RSC Med Chem 13: 1150-1196 (2022)
Prince Sattam Bin Abdulaziz University
-Methylamide-structured SB366791 derivatives with high TRPV1 antagonistic activity: toward PET radiotracers to visualize TRPV1.
RSC Med Chem 13: 1197-1204 (2022)
Riken Center For Biosystems Dynamics Research
Hydroxypyrone derivatives in drug discovery: from chelation therapy to rational design of metalloenzyme inhibitors.
RSC Med Chem 13: 1127-1149 (2022)
Government College Women University
Synthesis and biological evaluation of paeoveitol D derivatives as new melatonin receptor agonists with antidepressant activities.
RSC Med Chem 13: 1212-1224 (2022)
Chinese Academy of Sciences
4-Aminopyrazolopyrimidine scaffold and its deformation in the design of tyrosine and serine/threonine kinase inhibitors in medicinal chemistry.
RSC Med Chem 13: 1008-1028 (2022)
Yangtze University
New β-carboline derivatives containing imidazolium as potential VEGFR2 inhibitors: synthesis, X-ray structure, antiproliferative evaluations, and molecular modeling.
RSC Med Chem 13: 1064-1076 (2022)
University Shihezi
Orally Bioavailable Quinoxaline Inhibitors of 15-Prostaglandin Dehydrogenase (15-PGDH) Promote Tissue Repair and Regeneration.
J Med Chem 65: 15327-15343 (2022)
Ut Southwestern Medical Center
Discovery of Ervogastat (PF-06865571): A Potent and Selective Inhibitor of Diacylglycerol Acyltransferase 2 for the Treatment of Non-alcoholic Steatohepatitis.
J Med Chem 65: 15000-15013 (2022)
Pfizer
Interrogation of the Pathogen Box reveals small molecule ligands against the mycobacterial trehalose transporter LpqY-SugABC.
RSC Med Chem 13: 1225-1233 (2022)
University of Warwick
Discovery and Optimization of Indoline-Based Compounds as Dual 5-LOX/sEH Inhibitors:
J Med Chem 65: 14456-14480 (2022)
University Federico Ii of Naples
Discovery of Novel Pyrazolylpyridine Derivatives for 20-Hydroxyeicosatetraenoic Acid Synthase Inhibitors with Selective CYP4A11/4F2 Inhibition.
J Med Chem 65: 14599-14613 (2022)
Taisho Pharmaceutical
Conformationally Defined Rexinoids for the Prevention of Inflammation and Nonmelanoma Skin Cancers.
J Med Chem 65: 14409-14423 (2022)
TBA
Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
J Med Chem 65: 14326-14336 (2022)
Janssen Research & Development
1-Methyl-3-((4-(quinolin-4-yloxy)phenyl)amino)-1H-pyrazole-4-carboxamide derivatives as new rearranged during Transfection (RET) kinase inhibitors capable of suppressing resistant mutants in solvent-front regions.
Eur J Med Chem 244: (2022)
Jinan University
The inhibition of monoamine oxidase by 2H-1,4-benzothiazin-3(4H)-ones.
Bioorg Med Chem Lett 77: (2022)
North-West University
Selective butyrylcholinesterase inhibition by isatin dimers and 3-indolyl-3-hydroxy-2-oxindole dimers.
Bioorg Med Chem Lett 77: (2022)
The Behrend College
Development of a Highly Potent Transthyretin Amyloidogenesis Inhibitor: Design, Synthesis, and Evaluation.
J Med Chem 65: 14673-14691 (2022)
Universitat Aut£Noma De Barcelona
Discovery and characterization of novel potent BCR-ABL degraders by conjugating allosteric inhibitor.
Eur J Med Chem 244: (2022)
Shanghaitech University
Blocking Non-enzymatic Functions by PROTAC-Mediated Targeted Protein Degradation.
J Med Chem 65: 14276-14288 (2022)
Second Military Medical University (Naval Medical University)
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.
J Med Chem 65: 14764-14791 (2022)
University of Toledo
Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening.
J Med Chem 65: 14391-14408 (2022)
Glaxosmithkline
Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS
J Med Chem 65: 14614-14629 (2022)
Boehringer Ingelheim Rcv
Design, synthesis, and biological evaluation of 2-arylamino-4-(piperidin-4-yloxy)pyrimidines as potent EGFR
Bioorg Med Chem 74: (2022)
Shenyang Pharmaceutical University
Potent Uncompetitive Inhibitors of Nicotinamide
J Med Chem 65: 14642-14654 (2022)
Harvard University
Screening of a Halogen-Enriched Fragment Library Leads to Unconventional Binding Modes.
J Med Chem 65: 14539-14552 (2022)
Eberhard Karls Universit£T T£Bingen
Discovery of a Trifluoromethoxy Cyclopentanone Benzothiazole Receptor-Interacting Protein Kinase 1 Inhibitor as the Treatment for Alzheimer's Disease.
J Med Chem 65: 14957-14969 (2022)
China Pharmaceutical University
Callintegers A and B, Unusual Tricyclo[4.4.0.0
J Nat Prod 85: 2675-2681 (2022)
Yunnan Research & Development Center For Natural Products
Exploratory study of oxatomide derivatives with high P2X
Bioorg Med Chem Lett 77: (2022)
Takasaki University of Health and Welfare
Discovery of 4-methyl-3-(pyridin-2-ylamino)benzamide derivatives as C-Abl inhibitors with potential neuroprotective effect.
Bioorg Med Chem 74: (2022)
Southern Medical University
The SAR and action mechanisms of autophagy inhibitors that eliminate drug resistance.
Eur J Med Chem 244: (2022)
Guangzhou University of Chinese Medicine
From dopamine 4 to sigma 1: Synthesis, SAR and biological characterization of a piperidine scaffold of σ1 modulators.
Eur J Med Chem 244: (2022)
University of Nebraska Medical Center
Discovery of a Highly Potent and Orally Bioavailable STAT3 Dual Phosphorylation Inhibitor for Pancreatic Cancer Treatment.
J Med Chem 65: 15487-15511 (2022)
East China Normal University
Novel Aryl Alkamidazole Derivatives as Multifunctional Antifungal Inhibitors: Design, Synthesis, and Biological Evaluation.
J Med Chem 65: 14916-14937 (2022)
Liaocheng University
Novel alpha6 preferring GABA-A receptor ligands based on loreclezole.
Eur J Med Chem 244: (2022)
University of Vienna
Discovery and optimization of 4-anilinoquinazoline derivatives spanning ATP binding site and allosteric site as effective EGFR-C797S inhibitors.
Eur J Med Chem 244: (2022)
East China University of Science and Technology
Overcoming Preclinical Safety Obstacles to Discover (
J Med Chem 65: 14721-14739 (2022)
Jecure Therapeutics
Design, Synthesis, and Biological Evaluation of 5-Formyl-pyrrolo[3,2-
J Med Chem 65: 14809-14831 (2022)
Jinan University
Discovery of a NADPH oxidase inhibitor, (E)-3-cyclohexyl-5-(4-((2-hydroxyethyl)(methyl)amino)benzylidene)-1-methyl-2-thioxoimidazolidin-4-oneone, as a novel therapeutic for Parkinson's disease.
Eur J Med Chem 244: (2022)
Korea University
An overview of aryl hydrocarbon receptor ligands in the Last two decades (2002-2022): A medicinal chemistry perspective.
Eur J Med Chem 244: (2022)
China Pharmaceutical University
Medicinal chemistry strategies targeting PRMT5 for cancer therapy.
Eur J Med Chem 244: (2022)
Sichuan University
A bibliometric analysis of PROTAC from 2001 to 2021.
Eur J Med Chem 244: (2022)
First Affiliated Hospital of Gannan Medical University
Discovery of 5-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)-1H-indole-2-carboxamide derivatives as novel anti-cancer agents targeting Nur77.
Eur J Med Chem 244: (2022)
Xiamen University
Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.
Bioorg Med Chem 74: (2022)
Lanzhou University
Scaffold hopping via ring opening enables identification of acyclic compounds as new complement Factor D inhibitors.
Bioorg Med Chem 74: (2022)
Biocryst Pharmaceuticals
Discovery and Structure-Activity Relationship Studies of Novel Adenosine A
J Med Chem 65: 14864-14890 (2022)
University of Bern
Discovery and Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists
J Med Chem 65: 14843-14863 (2022)
Broad Institute of Mit and Harvard
Design, synthesis and biological evaluation of novel 4-aminopiperidine derivatives as SMO/ERK dual inhibitors.
Bioorg Med Chem 74: (2022)
China Pharmaceutical University
Discovery of selective covalent cathepsin K inhibitors containing novel 4-cyanopyrimidine warhead based on quantum chemical calculations and binding mode analysis.
Bioorg Med Chem 74: (2022)
China Pharmaceutical University
HIV-1 gp120-CXCR4 recognition probed with synthetic nanomolar affinity D-peptides containing fragments of gp120 V3 loop.
Eur J Med Chem 244: (2022)
Tsinghua University
Rational Design, Synthesis, and Biological Evaluation of Novel S1PR2 Antagonists for Reversing 5-FU-Resistance in Colorectal Cancer.
J Med Chem 65: 14553-14577 (2022)
Ocean University of China
New Dual P-Glycoprotein (P-gp) and Human Carbonic Anhydrase XII (hCA XII) Inhibitors as Multidrug Resistance (MDR) Reversers in Cancer Cells.
J Med Chem 65: 14655-14672 (2022)
University of Florence
Identification and Biochemical Characterization of Pyrrolidinediones as Novel Inhibitors of the Bacterial Enzyme MurA.
J Med Chem 65: 14740-14763 (2022)
Saarland University
Novel Lactams as Cbl-b Inhibitors for Treating Cancer.
ACS Med Chem Lett 13: 1556-1557 (2022)
Smith, Gambrell & Russell
Boron-Containing Pyrazole Compounds as JAK Inhibitors for Treating Inflammation, Autoimmune Diseases, and Cancer.
ACS Med Chem Lett 13: 1554-1555 (2022)
Smith, Gambrell & Russell
Factor XI Activation Inhibitors for Treating Thromboses, Embolism, Hypercoagulability, or Fibrotic Changes.
ACS Med Chem Lett 13: 1548-1549 (2022)
Smith, Gambrell & Russell
ALK Inhibitors for Treating Cancer, Blood, and Kidney Diseases.
ACS Med Chem Lett 13: 1539-1541 (2022)
Usona Institute
Selective Cyclin-Dependent Kinase Inhibitors and Their Application in Cancer Therapy.
ACS Med Chem Lett 13: 1561-1563 (2022)
Usona Institute
Novel Peptidylarginine Deiminase Type 4 (PAD4) Inhibitors.
ACS Med Chem Lett 13: 1537-1538 (2022)
Smith, Gambrell & Russell
Discovery of potent indazole-based human glutaminyl cyclase (QC) inhibitors as Anti-Alzheimer's disease agents.
Eur J Med Chem 244: (2022)
Seoul National University
Guanidine-based β amyloid precursor protein cleavage enzyme 1 (BACE-1) inhibitors for the Alzheimer's disease (AD): A review.
Bioorg Med Chem 74: (2022)
Central University of Rajasthan
The Pursuit of Enzyme Activation: A Snapshot of the Gold Rush.
J Med Chem 65: 14289-14304 (2022)
Baylor College of Medicine
Development of Noncovalent Small-Molecule Keap1-Nrf2 Inhibitors by Fragment-Based Drug Discovery.
J Med Chem 65: 14481-14526 (2022)
University of Copenhagen
Small Molecule Inhibitors of Lymphocyte Perforin as Focused Immunosuppressants for Infection and Autoimmunity.
J Med Chem 65: 14305-14325 (2022)
University of Auckland
Charting the Chemical Space of Acrylamide-Based Inhibitors of zDHHC20.
ACS Med Chem Lett 13: 1648-1654 (2022)
The University of Chicago
Pipeline Impact of Radiolabeled Compounds in Drug Discovery and Development.
ACS Med Chem Lett 13: 1564-1567 (2022)
Abbvie
Novel Substituted Cyclopropyl Compounds as CFTR Modulators for Treating Cystic Fibrosis.
ACS Med Chem Lett 13: 1552-1553 (2022)
Smith, Gambrell & Russell
Development of Esterase-Resistant and Highly Active Ghrelin Analogs via Thiol-Ene Click Chemistry.
ACS Med Chem Lett 13: 1655-1662 (2022)
Tongji University
Highly Potent and Oral Macrocyclic Peptides as a HIV-1 Protease Inhibitor: mRNA Display-Derived Hit-to-Lead Optimization.
ACS Med Chem Lett 13: 1634-1641 (2022)
Shionogi
Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates.
ACS Med Chem Lett 13: 1568-1573 (2022)
Kyoto Prefectural University of Medicine
Design, Synthesis, and Monoamine Oxidase B Selective Inhibitory Activity of
ACS Med Chem Lett 13: 1582-1590 (2022)
Osaka University
Synthesis and Structural Characterization of Novel Trihalo-sulfone Inhibitors of WNK1.
ACS Med Chem Lett 13: 1678-1684 (2022)
The University of Texas Southwestern Medical Center At Dallas
Development of an N-Terminal BRD4 Bromodomain-Targeted Degrader.
ACS Med Chem Lett 13: 1621-1627 (2022)
University of Minnesota
Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor.
ACS Med Chem Lett 13: 1591-1597 (2022)
Astex Pharmaceuticals
Design and Characterization of Novel Small Molecule Activators of Excitatory Amino Acid Transporter 2.
ACS Med Chem Lett 13: 1628-1633 (2022)
Drexel University College of Medicine
Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins.
ACS Med Chem Lett 13: 1574-1581 (2022)
Chinese Academy of Sciences
Amino-cyclohexane Carboxylic Acid Inhibitors of Arginase.
ACS Med Chem Lett 13: 1550-1551 (2022)
Arrival Discovery
BAY-069, a Novel (Trifluoromethyl)pyrimidinedione-Based BCAT1/2 Inhibitor and Chemical Probe.
J Med Chem 65: 14366-14390 (2022)
Bayer Pharma
Identification of 1,4-Benzodiazepine-2,5-dione Derivatives as Potential Protein Synthesis Inhibitors with Highly Potent Anticancer Activity.
J Med Chem 65: 14891-14915 (2022)
Tsinghua University
Discovery of novel hybrids containing clioquinol-1-benzyl-1,2,3,6-tetrahydropyridine as multi-target-directed ligands (MTDLs) against Alzheimer's disease.
Eur J Med Chem 244: (2022)
China Pharmaceutical University
Developing a Naïve Bayesian Classification Model with PI3Kγ structural features for virtual screening against PI3Kγ: Combining molecular docking and pharmacophore based on multiple PI3Kγ conformations.
Eur J Med Chem 244: (2022)
Jiangnan University
Therapeutic Activity of the Lansoprazole Metabolite 5-Hydroxy Lansoprazole Sulfide in Triple-Negative Breast Cancer by Inhibiting the Enoyl Reductase of Fatty Acid Synthase.
J Med Chem 65: 13681-13691 (2022)
Indiana University School of Medicine
Structure-Uptake Relationship Studies of Oxazolidinones in Gram-Negative ESKAPE Pathogens.
J Med Chem 65: 14144-14179 (2022)
University of Minnesota
Discovery of
J Med Chem 65: 14180-14200 (2022)
Helmholtz-Institute For Pharmaceutical Research Saarland (Hips)
Target-Focused Library Design by Pocket-Applied Computer Vision and Fragment Deep Generative Linking.
J Med Chem 65: 13771-13783 (2022)
Umr7200 Cnrs-Universit£
Novel combretastatin A-4 derivative containing aminophosphonates as dual inhibitors of tubulin and matrix metalloproteinases for lung cancer treatment.
Eur J Med Chem 244: (2022)
Huaiyin Institute of Technology
Prodrugs of a 1-Hydroxy-2-oxopiperidin-3-yl Phosphonate Enolase Inhibitor for the Treatment of
J Med Chem 65: 13813-13832 (2022)
University of Texas Md Anderson Cancer Center
Sebetralstat (KVD900): A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema.
J Med Chem 65: 13629-13644 (2022)
Kalvista Pharmaceuticals
Targeting Aggrecanases for Osteoarthritis Therapy: From Zinc Chelation to Exosite Inhibition.
J Med Chem 65: 13505-13532 (2022)
University of Pisa
A review of MMP-2 structures and binding mode analysis of its inhibitors to strategize structure-based drug design.
Bioorg Med Chem 74: (2022)
Adamas University
Rational design of metabolically stable HDAC inhibitors: An overhaul of trifluoromethyl ketones.
Eur J Med Chem 244: (2022)
University of Toledo
New β-arylchalcogeno amines with procognitive properties targeting Carbonic Anhydrases and Monoamine Oxidases.
Eur J Med Chem 244: (2022)
University of Florence
Design, synthesis, and properties of des-D-ring interphenylene derivatives of 1α,25-Dihydroxyvitamin D
Eur J Med Chem 243: (2022)
Kanagawa University
Discovery of a novel highly potent and low-toxic jatrophane derivative enhancing the P-glycoprotein-mediated doxorubicin sensitivity of MCF-7/ADR cells.
Eur J Med Chem 244: (2022)
Xinjiang Technical Institute of Physics & Chemistry
SAR studies toward discovery of emvododstat (PTC299), a potent dihydroorotate dehydrogenase (DHODH) inhibitor.
Eur J Med Chem 244: (2022)
Ptc USA
Synthesis, antitumor, and apoptosis-inducing activities of novel 5-arylidenethiazolidine-2,4-dione derivatives: Histone deacetylases inhibitory activity and molecular docking study.
Eur J Med Chem 244: (2022)
Mansoura University
Discovery of novel VEGFR-2-PROTAC degraders based on the localization of lysine residues via recruiting VHL for the treatment of gastric cancer.
Eur J Med Chem 244: (2022)
Lanzhou University
Single-digit nanomolar inhibitors lock the aromatase active site via a dualsteric targeting strategy.
Eur J Med Chem 244: (2022)
Alma Mater Studiorum-University of Bologna
Natural occurrence, bioactivity, and biosynthesis of triene-ansamycins.
Eur J Med Chem 244: (2022)
Second Military Medical University
Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease.
J Med Chem 65: 13852-13865 (2022)
Kyushu University
Discovery of a new class of valosine containing protein (VCP/P97) inhibitors for the treatment of colorectal cancer.
Bioorg Med Chem 74: (2022)
Nanjing Normal University
Design and characterization of PROTAC degraders specific to protein N-terminal methyltransferase 1.
Eur J Med Chem 244: (2022)
Kansas State University
Potent and Specific Activators for Mitochondrial Sirtuins Sirt3 and Sirt5.
J Med Chem 65: 14015-14031 (2022)
University of Bayreuth
Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening.
J Med Chem 65: 13714-13735 (2022)
Medical College of Wisconsin
Design, synthesis and evaluation of fused hybrids with acetylcholinesterase inhibiting and Nrf2 activating functions for Alzheimer's disease.
Eur J Med Chem 244: (2022)
China Pharmaceutical University
Synthesis and evaluation of small molecule inhibitors of LSD1 for use against MYCN-expressing neuroblastoma.
Eur J Med Chem 244: (2022)
Medical University of South Carolina
Synthesis, In Vitro Profiling, and In Vivo Evaluation of Benzohomoadamantane-Based Ureas for Visceral Pain: A New Indication for Soluble Epoxide Hydrolase Inhibitors.
J Med Chem 65: 13660-13680 (2022)
Universitat De Barcelona
Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer.
J Med Chem 65: 13645-13659 (2022)
Fudan University
Design, synthesis and activity evaluation of novel lesinurad analogues containing thienopyrimidinone or pyridine substructure as human urate transporter 1 inhibitors.
Eur J Med Chem 244: (2022)
Shandong University
Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of
J Med Chem 65: 14121-14143 (2022)
Ucb
Inhibition of glutathione S-transferases by photoactive calix[4]arene α-ketophosphonic acids.
Bioorg Med Chem Lett 77: (2022)
V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of The National Academy of Sciences of Ukraine
Targeting PGAM1 in cancer: An emerging therapeutic opportunity.
Eur J Med Chem 244: (2022)
Ningbo University
Synthesis and anticancer activity of novel histone deacetylase inhibitors that inhibit autophagy and induce apoptosis.
Eur J Med Chem 243: (2022)
Wuyi University
Fluorophenylalkyl-substituted cyanoguanidine derivatives as bacteria-selective MATE transporter inhibitors for the treatment of antibiotic-resistant infections.
Bioorg Med Chem 74: (2022)
Setsunan University
Proline based rationally designed peptide esters against dipeptidyl peptidase-4: Highly potent anti-diabetic agents.
Bioorg Med Chem Lett 76: (2022)
Guru Nanak Dev University
Zinc-dependent deacetylases (HDACs) as potential targets for treating Alzheimer's disease.
Bioorg Med Chem Lett 76: (2022)
Guizhou Medical University
Design and evaluation of novel analogs of 2-amino-4-boronobutanoic acid (ABBA) as inhibitors of human gamma-glutamyl transpeptidase.
Bioorg Med Chem 73: (2022)
State University of New York
Discovery and optimization of orally bioavailable and potent plasma Kallikrein inhibitors bearing a quaternary carbon.
Bioorg Med Chem 73: (2022)
Biocryst Pharmaceuticals
Recent Scaffold Hopping Applications in Central Nervous System Drug Discovery.
J Med Chem 65: 13483-13504 (2022)
The University of Sydney
Drug Hunting at the Nexus of Medicinal Chemistry and Chemical Biology and the Discovery of Novel Therapeutic Modalities.
J Med Chem 65: 13594-13613 (2022)
Novartis Institutes For Biomedical Research
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
J Med Chem 65: 13705-13713 (2022)
Cardiff University
Targeting Extracellular Signal-Regulated Protein Kinase 1/2 (ERK1/2) in Cancer: An Update on Pharmacological Small-Molecule Inhibitors.
J Med Chem 65: 13561-13573 (2022)
Southwest Jiaotong University
Natural Product-Inspired Targeted Protein Degraders: Advances and Perspectives.
J Med Chem 65: 13533-13560 (2022)
Tongji University School of Medicine
Discovery of BT8009: A Nectin-4 Targeting Bicycle Toxin Conjugate for the Treatment of Cancer.
J Med Chem 65: 14337-14347 (2022)
Bicycletx
Discovery, Chemistry, and Preclinical Development of Pritelivir, a Novel Treatment Option for Acyclovir-Resistant Herpes Simplex Virus Infections.
J Med Chem 65: 13614-13628 (2022)
Aicuris Anti-Infective Cures
Synthesis and antidepressant activity of novel 1-(1-benzoylpiperidin-4-yl) methanamine derivatives selectively targeting SSRI/5-HT
Bioorg Med Chem Lett 76: (2022)
Shanghai Institute of Pharmaceutical Industry
Development of a putative Zn
Bioorg Med Chem Lett 76: (2022)
Graz University of Technology
A comprehensive review of BET-targeting PROTACs for cancer therapy.
Bioorg Med Chem 73: (2022)
Xinxiang Medical University
Structure-activity relationships of mixed σ
Bioorg Med Chem 73: (2022)
University of Catania
Design and synthesis of functionalized 4-aryl-Catechol derivatives as new antiinflammtory agents with in vivo efficacy.
Eur J Med Chem 243: (2022)
University of Sannio
Development of benzene and benzothiazole-sulfonamide analogues as selective inhibitors of the tumor-associated carbonic anhydrase IX.
Eur J Med Chem 243: (2022)
Jamia Millia Islamia
Discovery of a Potent and Highly Selective Dipeptidyl Peptidase IV and Carbonic Anhydrase Inhibitor as "Antidiabesity" Agents Based on Repurposing and Morphing of WB-4101.
J Med Chem 65: 13946-13966 (2022)
University of Milan
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.
J Med Chem 65: 14082-14103 (2022)
Czech Academy of Sciences
Lectin-Targeted Prodrugs Activated by
J Med Chem 65: 13988-14014 (2022)
Helmholtz Institute For Pharmaceutical Research Saarland (Hips)
Discovery, Characterization, and Structure-Based Optimization of Small-Molecule In Vitro and In Vivo Probes for Human DNA Polymerase Theta.
J Med Chem 65: 13879-13891 (2022)
Artios Pharma
S-acylthioalkyl ester (SATE)-based prodrugs of deoxyribose cyclic dinucleotides (dCDNs) as the STING agonist for antitumor immunotherapy.
Eur J Med Chem 243: (2022)
Nankai University
Novel Allosteric Inhibitor-Derived AKT Proteolysis Targeting Chimeras (PROTACs) Enable Potent and Selective AKT Degradation in KRAS/BRAF Mutant Cells.
J Med Chem 65: 14237-14260 (2022)
Icahn School of Medicine At Mount Sinai
Structure-Based Design of Active-Site-Directed, Highly Potent, Selective, and Orally Bioavailable Low-Molecular-Weight Protein Tyrosine Phosphatase Inhibitors.
J Med Chem 65: 13892-13909 (2022)
Eli Lilly
Synthesis of capuramycin and its analogues via a Ferrier-type I reaction and their biological evaluation.
Bioorg Med Chem 73: (2022)
Hokkaido University
Discovery of novel compounds as potent activators of Sirt3.
Bioorg Med Chem 73: (2022)
Pmc Isochem
Discovery of 2-Methyl-2-(4-(2-methyl-8-(1
J Med Chem 65: 12781-12801 (2022)
West China Hospital of Sichuan University
Structure-activity relationship studies in a new series of 2-amino-N-phenylacetamide inhibitors of Slack potassium channels.
Bioorg Med Chem Lett 76: (2022)
University of North Texas Health Science Center
Structure-based design and modular synthesis of novel PI4K class II inhibitors bearing a 4-aminoquinazoline scaffold.
Bioorg Med Chem Lett 76: (2022)
Institute of Organic Chemistry and Biochemistry of The Czech Academy of Sciences
Design, synthesis, biological evaluation and molecular docking study of novel urea-based benzamide derivatives as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors.
Eur J Med Chem 243: (2022)
Sun Yat-Sen University
Recent advances of β-catenin small molecule inhibitors for cancer therapy: Current development and future perspectives.
Eur J Med Chem 243: (2022)
Sichuan University
Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3Kδ-selective template.
Bioorg Med Chem 73: (2022)
Anhui University of Chinese Medicine
Isatoic anhydrides as novel inhibitors of monoamine oxidase.
Bioorg Med Chem 73: (2022)
North-West University
Discovery of Pyrrolo[2,3-d]pyrimidine derivatives as potent and selective colony stimulating factor 1 receptor kinase inhibitors.
Eur J Med Chem 243: (2022)
Chinese Academy of Sciences
Alkyl-substituted N-methylaryl-N'-aryl-4-aminobenzamides: A new series of small molecule inhibitors for Wip1 phosphatase.
Eur J Med Chem 243: (2022)
Niddk
A systematic review on the kappa opioid receptor and its ligands: New directions for the treatment of pain, anxiety, depression, and drug abuse.
Eur J Med Chem 243: (2022)
University of Mississippi
Diastereomeric Resolution Yields Highly Potent Inhibitor of SARS-CoV-2 Main Protease.
J Med Chem 65: 13328-13342 (2022)
Bio-Techne (Tocris)
Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
J Med Chem 65: 13052-13073 (2022)
F. Hoffmann-La Roche
Probing Factor Xa Protein-Ligand Interactions: Accurate Free Energy Calculations and Experimental Validations of Two Series of High-Affinity Ligands.
J Med Chem 65: 13013-13028 (2022)
Leibniz-Forschungsinstitut F�R Molekulare Pharmakologie
Selective deuteration of bupropion slows epimerization and reduces metabolism.
Bioorg Med Chem Lett 76: (2022)
University of Washington
Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues.
Bioorg Med Chem Lett 76: (2022)
Tianjin Institute of Medical & Pharmaceutical Sciences
Identification and immunological evaluation of novel TLR2 agonists through structural optimization of Diprovocim.
Eur J Med Chem 243: (2022)
Fudan University
Structure-Based Optimization of Coumestan Derivatives as Polyketide Synthase 13-Thioesterase(Pks13-TE) Inhibitors with Improved hERG Profiles for
J Med Chem 65: 13240-13252 (2022)
East China Normal University
Development of MAO-A and 5-HT
J Med Chem 65: 13385-13400 (2022)
China Pharmaceutical University
Discovery of Isoform-Selective Akt3 Degraders Overcoming Osimertinib-Induced Resistance in Non-Small Cell Lung Cancer Cells.
J Med Chem 65: 14032-14048 (2022)
Jinan University
Dual A1/A3 Adenosine Receptor Antagonists: Binding Kinetics and Structure-Activity Relationship Studies Using Mutagenesis and Alchemical Binding Free Energy Calculations.
J Med Chem 65: 13305-13327 (2022)
National and Kapodistrian University of Athens
Discovery of Orally Bioavailable SOS1 Inhibitors for Suppressing KRAS-Driven Carcinoma.
J Med Chem 65: 13158-13171 (2022)
Wuhan University of Science and Technology
Design, synthesis, and biological evaluation of Wee1 kinase degraders.
Eur J Med Chem 243: (2022)
East China Normal University
Bisindole natural products: A vital source for the development of new anticancer drugs.
Eur J Med Chem 243: (2022)
Hubei University of Science and Technology
Boronic Acid: A Novel Pharmacophore Targeting Src Homology 2 (SH2) Domain of STAT3.
J Med Chem 65: 13094-13111 (2022)
Sun Yat-Sen University
Linker-Dependent Folding Rationalizes PROTAC Cell Permeability.
J Med Chem 65: 13029-13040 (2022)
Uppsala University
Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia.
J Med Chem 65: 13436-13451 (2022)
Southeast University
Targeting SARS-CoV-2 Main Protease for Treatment of COVID-19: Covalent Inhibitors Structure-Activity Relationship Insights and Evolution Perspectives.
J Med Chem 65: 12500-12534 (2022)
University of Palermo
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
J Med Chem 65: 12956-12969 (2022)
The University of Queensland
Recent two-year advances in anti-dengue small-molecule inhibitors.
Eur J Med Chem 243: (2022)
Macao University of Science and Technology
Identification of Novel 2,4,5-Trisubstituted Pyrimidines as Potent Dual Inhibitors of Plasmodial
J Med Chem 65: 13172-13197 (2022)
University of North Carolina at Chapel Hill
Design, Synthesis, Biological Activity, and Structural Analysis of Novel Des-C-Ring and Aromatic-D-Ring Analogues of 1α,25-Dihydroxyvitamin D
J Med Chem 65: 13112-13124 (2022)
University of Santiago De Compostela
Piptide Chemotypes for Perturbation of the Interaction of Urokinase with Its Receptor.
J Med Chem 65: 12925-12932 (2022)
Texas A&M University
Design, synthesis, in-vitro, in-vivo and ex-vivo pharmacology of thiazolidine-2,4-dione derivatives as selective and reversible monoamine oxidase-B inhibitors.
Bioorg Med Chem Lett 76: (2022)
Comsats University Islamabad
Discovery of a novel piperlongumine analogue as a microtubule polymerization inhibitor with potent anti-angiogenic and anti-metastatic efficacy.
Eur J Med Chem 243: (2022)
Zhengzhou University
Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-
J Med Chem 65: 12701-12724 (2022)
University of Turin
Review of bioactivity and structure-activity relationship on baicalein (5,6,7-trihydroxyflavone) and wogonin (5,7-dihydroxy-8-methoxyflavone) derivatives: Structural modifications inspired from flavonoids in Scutellaria baicalensis.
Eur J Med Chem 243: (2022)
Shaanxi University of Chinese Medicine
A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.
Eur J Med Chem 243: (2022)
China Pharmaceutical University
Discovery and Optimization of the First Highly Effective and Orally Available Galectin-3 Inhibitors for Treatment of Fibrotic Disease.
J Med Chem 65: 12626-12638 (2022)
Galecto Biotech
Discovery and Characterization of Synthesized and FDA-Approved Inhibitors of Clostridial and Bacillary Collagenases.
J Med Chem 65: 12933-12955 (2022)
Helmholtz Center For Infection Research (Hzi)
Discovery of 2-(1-(3-Chloro-4-cyanophenyl)-1
J Med Chem 65: 13074-13093 (2022)
Zhejiang University
Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.
J Med Chem 65: 12838-12859 (2022)
China Pharmaceutical University
A high quality, industrial data set for binding affinity prediction: performance comparison in different early drug discovery scenarios.
J Comput Aided Mol Des 36: 753-765 (2022)
F. Hoffmann-La Roche
Current medicinal chemistry strategies in the discovery of novel HIV-1 ribonuclease H inhibitors.
Eur J Med Chem 243: (2022)
Shandong University
Ad-hoc modifications of cyclic mimetics of SOCS1 protein: Structural and functional insights.
Eur J Med Chem 243: (2022)
University of Naples "Federico Ii
Discovery of biphenyls bearing thiobarbiturate fragment by structure-based strategy as Mycobacterium tuberculosis protein tyrosine phosphatase B inhibitors.
Bioorg Med Chem 73: (2022)
Peking Union Medical College and Chinese Academy of Medical Sciences
Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors.
Bioorg Med Chem 73: (2022)
Southern Medical University
2-Arylmelatonin analogues: Probing the 2-phenyl binding pocket of melatonin MT
Eur J Med Chem 243: (2022)
University of Urbino Carlo Bo
Structure-Activity Relationship and Neuroprotective Activity of 1,5-Dihydro-2
J Med Chem 65: 13967-13987 (2022)
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery and Development of First-in-Class ACKR3/CXCR7 Superagonists for Platelet Degranulation Modulation.
J Med Chem 65: 13365-13384 (2022)
Eberhard Karls University T£Bingen
Chemical Toolkit for PARK7: Potent, Selective, and High-Throughput.
J Med Chem 65: 13288-13304 (2022)
Leiden University Medical Center
New potent ciprofloxacin-uracil conjugates as DNA gyrase and topoisomerase IV inhibitors against methicillin-resistant Staphylococcus aureus.
Bioorg Med Chem 73: (2022)
Al-Azhar University
Multi-parameter optimization: Development of a morpholin-3-one derivative with an improved kinetic profile for imaging monoacylglycerol lipase in the brain.
Eur J Med Chem 243: (2022)
Eth Zurich
Subtilisin-like Serine Protease 1 (SUB1) as an Emerging Antimalarial Drug Target: Current Achievements in Inhibitor Discovery.
J Med Chem 65: 12535-12545 (2022)
Latvian Institute of Organic Synthesis
Discovery of Highly Potent and Selective Matrix Metalloproteinase-7 Inhibitors by Hybridizing the S1' Subsite Binder with Short Peptides.
J Med Chem 65: 13253-13263 (2022)
Taisho Pharmaceutical
Mechanism of Action and Structure-Activity Relationship of α-Conotoxin Mr1.1 at the Human α9α10 Nicotinic Acetylcholine Receptor.
J Med Chem 65: 16204-16217 (2022)
Ocean University of China
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
J Med Chem 65: 13264-13287 (2022)
Johann Wolfgang Goethe-University
Design, synthesis and biological evaluations of novel farnesoid X receptor (FXR) agonists.
Bioorg Med Chem Lett 76: (2022)
Shandong University
Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors.
Bioorg Med Chem Lett 76: (2022)
East China University of Science & Technology
Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy.
J Med Chem 65: 12895-12924 (2022)
Rapt Therapeutics
Biphenyl-based small molecule inhibitors: Novel cancer immunotherapeutic agents targeting PD-1/PD-L1 interaction.
Bioorg Med Chem 73: (2022)
Acharya & Bm Reddy College of Pharmacy
Covalent inhibitors of bacterial peptidoglycan biosynthesis enzyme MurA with chloroacetamide warhead.
Eur J Med Chem 243: (2022)
University of Ljubljana
A close look into the biological and synthetic aspects of fused pyrazole derivatives.
Eur J Med Chem 243: (2022)
Chengdu University of Traditional Chinese Medicine
Bioactive Aurones, Indanones, and Other Hemiindigoid Scaffolds: Medicinal Chemistry and Photopharmacology Perspectives.
J Med Chem 65: 12594-12625 (2022)
Universite Grenoble Alpes
Design and Synthesis of a 2-Amino-pyridine Derivative as a Potent CDK8 Inhibitor for Anti-colorectal Cancer Therapy.
J Med Chem 65: 13216-13239 (2022)
Anhui Medical University
Discovery of Phenolic Matrix Metalloproteinase Inhibitors by Peptide Microarray for Osteosarcoma Treatment.
J Nat Prod 85: 2424-2432 (2022)
Chinese Academy of Sciences
Development of Hydrogen Sulfide-Releasing Carbonic Anhydrases IX- and XII-Selective Inhibitors with Enhanced Antihyperalgesic Action in a Rat Model of Arthritis.
J Med Chem 65: 13143-13157 (2022)
University of Firenze
Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4.
J Med Chem 65: 12725-12746 (2022)
Lunenfeld-Tanenbaum Research Institute
Discovery of the 4-aminopiperidine-based compound EM127 for the site-specific covalent inhibition of SMYD3.
Eur J Med Chem 243: (2022)
Institute of Organic Synthesis and Photoreactivity - National Research Council
Boosting caffeic acid performance as antioxidant and monoamine oxidase B/catechol-O-methyltransferase inhibitor.
Eur J Med Chem 243: (2022)
University of Porto
Defining the structure-activity relationship for a novel class of allosteric MKP5 inhibitors.
Eur J Med Chem 243: (2022)
Yale University
Discovery of potent human dihydroorotate dehydrogenase inhibitors based on a benzophenone scaffold.
Eur J Med Chem 243: (2022)
Sichuan University
Fragment-based discovery of novel phenyltriazolyl derivatives as allosteric type-I
Bioorg Med Chem Lett 75: (2022)
Shenyang Pharmaceutical University
A simplified analog of debromoaplysiatoxin lacking the B-ring of spiroketal moiety retains protein kinase C-binding and antiproliferative activities.
Bioorg Med Chem 73: (2022)
Kagawa University
Discovery of Novel Pyrazole-Based KDM5B Inhibitor
J Med Chem 65: 12979-13000 (2022)
Zhengzhou University
Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of β-Coronaviruses.
J Med Chem 65: 12860-12882 (2022)
University of North Carolina at Chapel Hill
Inhibiting Sodium Taurocholate Cotransporting Polypeptide in HBV-Related Diseases: From Biological Function to Therapeutic Potential.
J Med Chem 65: 12546-12561 (2022)
Southwest Jiaotong University
Fragment Ligands of the m
ACS Med Chem Lett 13: 1500-1509 (2022)
University of Zurich
Synthesis, binding affinity, and inhibitory capacity of cyclodextrin-based multivalent glycan ligands for human galectin-3.
Bioorg Med Chem 72: (2022)
University of Maryland
Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity.
J Med Chem 65: 13343-13364 (2022)
Shandong University
Discovery of Betulinic Acid Derivatives as Potent Intestinal Farnesoid X Receptor Antagonists to Ameliorate Nonalcoholic Steatohepatitis.
J Med Chem 65: 13452-13472 (2022)
Chinese Academy of Sciences
Novel Coronavirus Main Protease Di- and Tripeptide Inhibitors for Treating COVID-19.
ACS Med Chem Lett 13: 1388-1389 (2022)
Experimental Drug Development Centre
Stereoisomers of an Aryl Pyrazole Glucocorticoid Receptor Agonist Scaffold Elicit Differing Anti-inflammatory Responses.
ACS Med Chem Lett 13: 1493-1499 (2022)
University of Tennessee
Oral Nonpeptidic, Noncovalent Triazine Coronavirus Main Protease Inhibitors for Treating COVID-19.
ACS Med Chem Lett 13: 1394-1396 (2022)
Experimental Drug Development Centre
Substituted 6,7-Dihydro-5
ACS Med Chem Lett 13: 1392-1393 (2022)
Smith, Gambrell & Russell
2-Amino-1,3,4-thiadiazoles as Glutaminyl Cyclases Inhibitors Increase Phagocytosis through Modification of CD47-SIRPα Checkpoint.
ACS Med Chem Lett 13: 1459-1467 (2022)
Ewha Womans University
Identification of a BAZ2A-Bromodomain Hit Compound by Fragment Growing.
ACS Med Chem Lett 13: 1434-1443 (2022)
University of Trento
Restoration of Motor Function Post-Neurological Injury Using Serotonergic Agonist.
ACS Med Chem Lett 13: 1397-1399 (2022)
Usona Institute
Orexin Receptor Agonists as Possible Treatment for Narcolepsy and Idiopathic Hypersomnia.
ACS Med Chem Lett 13: 1411-1412 (2022)
Therachem Research Medilab
Novel Bcl-2 Inhibitors Selectively Disrupt the Autophagy-Specific Bcl-2-Beclin 1 Protein-Protein Interaction.
ACS Med Chem Lett 13: 1510-1516 (2022)
University of Texas Southwestern Medical Center
Multicomponent Macrocyclic IL-17a Modifier.
ACS Med Chem Lett 13: 1468-1471 (2022)
University of Groningen
Biological Effects of Modifications of the Englerin A Glycolate.
ACS Med Chem Lett 13: 1472-1476 (2022)
National Cancer Institute
Novel 3-Aminopyrrolidine and Piperidine Macrocyclic Orexin Receptor Agonists for Treating Sleep Disorders.
ACS Med Chem Lett 13: 1390-1391 (2022)
Smith, Gambrell & Russell
Structure-Activity Relationship and
ACS Med Chem Lett 13: 1485-1492 (2022)
Riken Center For Biosystems Dynamics Research
Discovery of a Novel Potent STAT3 Inhibitor HP590 with Dual p-Tyr
J Med Chem 65: 12650-12674 (2022)
East China Normal University
X-ray Screening of an Electrophilic Fragment Library and Application toward the Development of a Novel ERK 1/2 Covalent Inhibitor.
J Med Chem 65: 12319-12333 (2022)
Astex Pharmaceuticals
Discovery of BET specific bromodomain inhibitors with a novel scaffold.
Bioorg Med Chem 72: (2022)
University of Science & Technology
Discovery of β-Arrestin-Biased 25CN-NBOH-Derived 5-HT
J Med Chem 65: 12031-12043 (2022)
University of Copenhagen
The Design, Synthesis, and Evaluation of Novel 9-Arylxanthenedione-Based Allosteric Modulators for the δ
J Med Chem 65: 12367-12385 (2022)
Monash University (Parkville Campus)
Naturally Occurring Partially Reduced Perylenequinones from Fungi.
J Nat Prod 85: 2236-2250 (2022)
Universidade Federal Da Bahia
Highly Potent and Selective Dopamine D
J Med Chem 65: 12124-12139 (2022)
University of Camerino
The Natural Products Withaferin A and Withanone from the Medicinal Herb
J Nat Prod 85: 2340-2350 (2022)
Shiv Nadar University
Developing HDAC4-Selective Protein Degraders To Investigate the Role of HDAC4 in Huntington's Disease Pathology.
J Med Chem 65: 12445-12459 (2022)
Charles River Laboratories
Bisubstrate Inhibitors of Severe Acute Respiratory Syndrome Coronavirus-2 Nsp14 Methyltransferase.
ACS Med Chem Lett 13: 1477-1484 (2022)
University of Minnesota
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.
J Med Chem 65: 12200-12218 (2022)
Shandong University
Development of selective FGFR1 degraders using a Rapid synthesis of proteolysis targeting Chimera (Rapid-TAC) platform.
Bioorg Med Chem Lett 75: (2022)
University of Wisconsin-Madison
Pseudoprolines as stereoelectronically tunable proline isosteres.
Bioorg Med Chem Lett 75: (2022)
Bristol Myers Squibb
Identification of novel piperazine-tethered phthalazines as selective CDK1 inhibitors endowed with in vitro anticancer activity toward the pancreatic cancer.
Eur J Med Chem 243: (2022)
Kafrelsheikh University
Design, synthesis and anti-tumor efficacy of novel phenyl thiazole/triazole derivatives as selective TrkA inhibitors.
Bioorg Med Chem 72: (2022)
Shenyang Pharmaceutical University
Spiroisoxazoline Inhibitors of Acetylcholinesterase from
J Nat Prod 85: 2207-2216 (2022)
University of Riau
A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia.
J Med Chem 65: 12014-12030 (2022)
Newcastle University
Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model.
RSC Med Chem 13: 944-954 (2022)
Julius Maximilian University of W�Rzburg
Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads.
RSC Med Chem 13: 963-969 (2022)
University of Maryland
Recent applications of covalent chemistries in protein-protein interaction inhibitors.
RSC Med Chem 13: 921-928 (2022)
University of Maryland
Development of tumor-targeting aza-vesamicol derivatives with high affinity for sigma receptors for cancer theranostics.
RSC Med Chem 13: 986-997 (2022)
Kanazawa University
Design and Characterization of a Natural Arf-GEFs Inhibitor Prodrug
J Med Chem 65: 11970-11984 (2022)
Ocean University of China
Synthesis and pharmacological characterization of multiply substituted 2H-chromene derivatives as P2Y
Bioorg Med Chem Lett 75: (2022)
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery and preclinical evaluations of GST-HG131, a novel HBV antigen inhibitor for the treatment of chronic hepatitis B infection.
Bioorg Med Chem Lett 75: (2022)
Wuxi Apptec
Discovery of MDV6058 (PF-06952229), a selective and potent TGFβR1 inhibitor: Design, synthesis and optimization.
Bioorg Med Chem Lett 75: (2022)
Integral Biosciences
Ligand- and structure-based identification of novel CDK9 inhibitors for the potential treatment of leukemia.
Bioorg Med Chem 72: (2022)
South China University of Technology
Design, synthesis, and biological evaluation of aromatic tertiary amine derivatives as selective butyrylcholinesterase inhibitors for the treatment of Alzheimer's disease.
Eur J Med Chem 243: (2022)
China Pharmaceutical University
Benzo[b]thiophene-2-carboxamides as novel opioid receptor agonists with potent analgesic effect and reduced constipation.
Eur J Med Chem 243: (2022)
National Health Research Institutes
Design, Synthesis, and Biological Evaluation of New 1H-Imidazole-2-Carboxylic Acid Derivatives as Metallo-β-Lactamase Inhibitors.
Bioorg Med Chem 72: (2022)
Xihua University
Discovery of Potent Cholinesterase Inhibition-Based Multi-Target-Directed Lead Compounds for Synaptoprotection in Alzheimer's Disease.
J Med Chem 65: 12292-12318 (2022)
Yeditepe University
Development of Inhibitors Targeting the V-Domain Ig Suppressor of T Cell Activation Signal Pathway.
J Med Chem 65: 11900-11912 (2022)
China Pharmaceutical University
Discovery of pyrrolo[2,3-d]pyrimidine-based molecules as a Wee1 inhibitor template.
Bioorg Med Chem Lett 75: (2022)
Capital Medical University
Discovery of pimozide derivatives as novel T-type calcium channel inhibitors with little binding affinity to dopamine D
Eur J Med Chem 243: (2022)
Kindai University
Cyclic Peptide Screening Methods for Preclinical Drug Discovery.
J Med Chem 65: 11913-11926 (2022)
University of Washington
Design, Synthesis, and Biological Evaluation of Dual-Target COX-2/CYP51 Inhibitors for the Treatment of Fungal Infectious Diseases.
J Med Chem 65: 12219-12239 (2022)
Liaocheng University
Venglustat Inhibits Protein N-Terminal Methyltransferase 1 in a Substrate-Competitive Manner.
J Med Chem 65: 12334-12345 (2022)
Purdue University
First-in-Class Hydrazide-Based HDAC6 Selective Inhibitor with Potent Oral Anti-Inflammatory Activity by Attenuating NLRP3 Inflammasome Activation.
J Med Chem 65: 12140-12162 (2022)
Ocean University of China
Chemo- and Site-Selective Lysine Modification of Peptides and Proteins under Native Conditions Using the Water-Soluble Zolinium.
J Med Chem 65: 11840-11853 (2022)
Chinese Academy of Sciences
Design, Synthesis, and Biological Evaluation of Androgen Receptor Degrading and Antagonizing Bifunctional Steroidal Analogs for the Treatment of Advanced Prostate Cancer.
J Med Chem 65: 12460-12481 (2022)
Shanghai Institute of Materia Medica
Discovery of Selenium-Containing STING Agonists as Orally Available Antitumor Agents.
J Med Chem 65: 15048-15065 (2022)
China Pharmaceutical University
Magnet for the Needle in Haystack: "Crystal Structure First" Fragment Hits Unlock Active Chemical Matter Using Targeted Exploration of Vast Chemical Spaces.
J Med Chem 65: 15663-15678 (2022)
Crystalsfirst
Paradoxical Increase of Permeability and Lipophilicity with the Increasing Topological Polar Surface Area within a Series of PRMT5 Inhibitors.
J Med Chem 65: 12386-12402 (2022)
Novartis Institutes For Biomedical Research
Discovery of the Novel 1
J Med Chem 65: 12095-12123 (2022)
Anhui Medical University
Combination of NSAIDs with donepezil as multi-target directed ligands for the treatment of Alzheimer's disease.
Bioorg Med Chem Lett 75: (2022)
Southeast University
Discovery of Cyclic Peptide Inhibitors Targeting PD-L1 for Cancer Immunotherapy.
J Med Chem 65: 12002-12013 (2022)
University of Missouri-Kansas City
Discovery of CH7057288 as an Orally Bioavailable, Selective, and Potent pan-TRK Inhibitor.
J Med Chem 65: 12427-12444 (2022)
Chugai Pharmaceutical
A guanidinium group is an effective mimic of the tertiary carbocation formed by isopentenyl diphosphate isomerase.
Bioorg Med Chem Lett 75: (2022)
University of British Columbia
Design, synthesis and biological evaluation of novel macrocyclic derivatives bearing aniline pyrimidine scaffolds as EGFR-TKIs.
Bioorg Med Chem Lett 75: (2022)
China State Institute of Pharmaceutical Industry Co.
Structure-based discovery of 1-(3-fluoro-5-(5-(3-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)phenyl)-3-(pyrimidin-5-yl)urea as a potent and selective nanomolar type-II PLK4 inhibitor.
Eur J Med Chem 243: (2022)
Shenyang Pharmaceutical University
Discovery of 1,2-diphenylethene derivatives as human DNA topoisomerase II catalytic inhibitors and antitumor agents.
Eur J Med Chem 243: (2022)
Shandong University
A chemical perspective on the modulation of TEAD transcriptional activities: Recent progress, challenges, and opportunities.
Eur J Med Chem 243: (2022)
Shanghai Institute of Materia Medica
Catalytic covalent inhibition of cyclooxygenase-1 by a biomimetic acyltransferase.
Bioorg Med Chem 72: (2022)
University of Delaware
Chemical similarities and differences among inhibitors of nitric oxide synthase, arginase and dimethylarginine dimethylaminohydrolase-1: Implications for the design of novel enzyme inhibitors modulating the nitric oxide pathway.
Bioorg Med Chem 72: (2022)
Flinders University
Discovery of a Novel Oral Proteasome Inhibitor to Block NLRP3 Inflammasome Activation with Anti-inflammation Activity.
J Med Chem 65: 11985-12001 (2022)
Guangzhou Medical University
From a Cone Snail Toxin to a Competitive MC4R Antagonist.
J Med Chem 65: 12084-12094 (2022)
Paris-Saclay University
Design, synthesis, and structure-activity relationship of novel RIPK2 inhibitors.
Bioorg Med Chem Lett 75: (2022)
Soochow University
Recent progress toward developing axial chirality bioactive compounds.
Eur J Med Chem 243: (2022)
Shandong University
Design, synthesis, and pharmacological evaluation of 2-(1-(1,3,4-thiadiazol-2-yl)piperidin-4-yl)ethan-1-ol analogs as novel glutaminase 1 inhibitors.
Eur J Med Chem 243: (2022)
Sichuan University
Discovery of dehydroandrographolide derivatives with C19 hindered ether as potent anti-ZIKV agents with inhibitory activities to MTase of ZIKV NS5.
Eur J Med Chem 243: (2022)
Nanjing Tech University
The current strategies of optimization of oseltamivir against mutant neuraminidases of influenza A：A review.
Eur J Med Chem 243: (2022)
Shenyang Pharmaceutical University
Targeting GRK2 and GRK5 for treating chronic degenerative diseases: Advances and future perspectives.
Eur J Med Chem 243: (2022)
West China Hospital
Development and structure-activity relationship of tacrine derivatives as highly potent CDK2/9 inhibitors for the treatment of cancer.
Eur J Med Chem 242: (2022)
Shenyang Pharmaceutical University
Discovery of Novel Imidazo[4,5-
J Med Chem 65: 11949-11969 (2022)
Chinese Academy of Sciences
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.
J Med Chem 65: 12346-12366 (2022)
Sun Yat-Sen University
Discovery of a novel photoswitchable PI3K inhibitor toward optically-controlled anticancer activity.
Bioorg Med Chem 72: (2022)
Peking Union Medical College
Discovery of azaspirocyclic 1H-3,4,5-Trisubstitued pyrazoles as novel G2019S-LRRK2 selective kinase inhibitors.
Eur J Med Chem 242: (2022)
Stanford University
Development of 3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-sulfate sodium salt (INT-767): Process optimization, synthesis and characterization of metabolites.
Eur J Med Chem 242: (2022)
University of Perugia
Zamamiphidins B and C, Manzamine-Related Alkaloids from an
J Nat Prod 85: 2226-2231 (2022)
Showa Pharmaceutical University
Recent advance on pleiotropic cholinesterase inhibitors bearing amyloid modulation efficacy.
Eur J Med Chem 242: (2022)
University of South China
2-(Fluoromethoxy)-4'-(
J Med Chem 65: 12256-12272 (2022)
Universidad Complutense De Madrid
The Discovery of GSK3640254, a Next-Generation Inhibitor of HIV-1 Maturation.
J Med Chem 65: 11927-11948 (2022)
Bristol Myers Squibb Research and Early Development
Novel allosteric glutaminase 1 inhibitors with macrocyclic structure activity relationship analysis.
Bioorg Med Chem Lett 75: (2022)
Yonsei University College of Medicine
Discovery of substituted benzyloxy-benzylamine inhibitors of acetyltransferase Eis and their anti-mycobacterial activity.
Eur J Med Chem 242: (2022)
University of Kentucky
Monoamine oxidase inhibitors: A concise review with special emphasis on structure activity relationship studies.
Eur J Med Chem 242: (2022)
Guru Jambheshwar University of Science and Technology
Discovery of IHMT-MST1-58 as a Novel, Potent, and Selective MST1 Inhibitor for the Treatment of Type 1/2 Diabetes.
J Med Chem 65: 11818-11839 (2022)
Chinese Academy of Sciences
The discovery of BMS-737 as a potent, CYP17 lyase-selective inhibitor for the treatment of castration-resistant prostate cancer.
Bioorg Med Chem Lett 75: (2022)
Bristol-Myers Squibb
Identification of the gossypol derivatives as androgen receptor inhibitor.
Bioorg Med Chem Lett 75: (2022)
Zhejiang Normal University
1,2,4-Triazole-3-thione analogues with an arylakyl group at position 4 as metallo-β-lactamase inhibitors.
Bioorg Med Chem 72: (2022)
Cnrs
Targeting non-alcoholic fatty liver disease: Design, X-ray co-crystal structure and synthesis of 'first-in-kind' inhibitors of serine/threonine kinase25.
Bioorg Med Chem Lett 75: (2022)
University of Montreal
Design and exploration of gut-restricted bifunctional molecule with TGR5 agonistic and DPP4 inhibitory effects for treating ulcerative colitis.
Eur J Med Chem 242: (2022)
Shanghai Institute of Materia Medica
Discovery of novel non-nucleoside inhibitors with high potency and selectivity for DNA methyltransferase 3A.
Eur J Med Chem 242: (2022)
Zhejiang University
Novel cudraisoflavone J derivatives as potent neuroprotective agents for the treatment of Parkinson's disease via the activation of Nrf2/HO-1 signaling.
Eur J Med Chem 242: (2022)
Dongguk University-Seoul
Discovery of Potent and Selective Transient Receptor Potential Vanilloid 1 (TRPV1) Agonists with Analgesic Effects
J Med Chem 65: 11658-11678 (2022)
Fudan University
Design, synthesis and biological evaluation of novel coumarin derivatives as multifunctional ligands for the treatment of Alzheimer's disease.
Eur J Med Chem 242: (2022)
Shenyang Pharmaceutical University
Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities.
J Med Chem 65: 11745-11758 (2022)
Sun Yat-Sen University
Discovery of AZD4831, a Mechanism-Based Irreversible Inhibitor of Myeloperoxidase, As a Potential Treatment for Heart Failure with Preserved Ejection Fraction.
J Med Chem 65: 11485-11496 (2022)
Astrazeneca
Discovery of novel benzbromarone analogs with improved pharmacokinetics and benign toxicity profiles as antihyperuricemic agents.
Eur J Med Chem 242: (2022)
Southern Medical University
Exploring gabosine and chlorogentisyl alcohol derivatives from a marine-derived fungus as EcGUS inhibitors with informatic assisted approaches.
Eur J Med Chem 242: (2022)
Zhejiang University
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