286 articles for thisTarget
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Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines.
Glaxosmithkline
Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity.
University of Bath
Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors.
Health & Science University
Structure-activity relationships of 2-arylquinazolin-4-ones as highly selective and potent inhibitors of the tankyrases.
University of Bath
Potential Use of Inhibitors of Tankyrases and PARP-1 as Treatment for Cancer and Other Diseases.
Therachem Research Medilab (India)
Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) Polymerase-1/2 Inhibitor, as an Anticancer Agent.
Biomarin Pharmaceutical
Development and structural analysis of adenosine site binding tankyrase inhibitors.
University of Oulu
Selective inhibition of PARP10 using a chemical genetics strategy.
Oregon Health & Science University
Identification of novel PARP-1 inhibitors: Drug design, synthesis and biological evaluation.
China Pharmaceutical University
Recent developments regarding the use of thieno[2,3-d]pyrimidin-4-one derivatives in medicinal chemistry, with a focus on their synthesis and anticancer properties.
Xinjiang Technical Institute of Physics and Chemistry
Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.
Nerviano Medical Sciences
Discovery of potent and selective nonplanar tankyrase inhibiting nicotinamide mimics.
University of Oulu
Benzimidazole derivatives as potential dual inhibitors for PARP-1 and DHODH.
University of Malaya
Structure-based design, synthesis and evaluation in vitro of arylnaphthyridinones, arylpyridopyrimidinones and their tetrahydro derivatives as inhibitors of the tankyrases.
University of Bath
Tankyrase 1 Inhibitors with Drug-like Properties Identified by Screening a DNA-Encoded Chemical Library.
Philochem
Niraparib: A Poly(ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination.
Istituto Di Ricerche Di Biologia Molecolare
Design, synthesis and biological evaluation of pyridazino[3,4,5-de]quinazolin-3(2H)-one as a new class of PARP-1 inhibitors.
Peking University
Towards small molecule inhibitors of mono-ADP-ribosyltransferases.
Karolinska Institutet
Synthesis and biological evaluation of isoindoloisoquinolinone, pyroloisoquinolinone and benzoquinazolinone derivatives as poly(ADP-ribose) polymerase-1 inhibitors.
Pondicherry University
Synthesis and biological evaluation of substituted 4-(thiophen-2-ylmethyl)-2H-phthalazin-1-ones as potent PARP-1 inhibitors.
Beijing Institute of Pharmacology and Toxicology
Discovery and structure-activity relationship of novel 2,3-dihydrobenzofuran-7-carboxamide and 2,3-dihydrobenzofuran-3(2H)-one-7-carboxamide derivatives as poly(ADP-ribose)polymerase-1 inhibitors.
St. John'S University
Synthesis of isoquinolinone-based tricycles as novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors.
Chinese Academy of Sciences
Design, synthesis, crystallographic studies, and preliminary biological appraisal of new substituted triazolo[4,3-b]pyridazin-8-amine derivatives as tankyrase inhibitors.
University of Perugia
Nitric oxide (NO) releasing poly ADP-ribose polymerase 1 (PARP-1) inhibitors targeted to glutathione S-transferase P1-overexpressing cancer cells.
National Cancer Institute-Frederick
Synthesis, [¹8F] radiolabeling, and evaluation of poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors for in vivo imaging of PARP-1 using positron emission tomography.
Washington University Saint Louis
Evaluation and Structural Basis for the Inhibition of Tankyrases by PARP Inhibitors.
University of Oulu
Novel PARP-1 inhibitors based on a 2-propanoyl-3H-quinazolin-4-one scaffold.
R&D Sigma-Tau Industrie Farmaceutiche Riunite
Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.
Amgen
Design and Discovery of 2-Arylquinazolin-4-ones as Potent and Selective Inhibitors of Tankyrases.
University of Bath
Chemical probes to study ADP-ribosylation: synthesis and biochemical evaluation of inhibitors of the human ADP-ribosyltransferase ARTD3/PARP3.
Ume£
Identification of novel PARP-1 inhibitors by structure-based virtual screening.
St. John'S University
Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity.
University of Oulu
Structure-efficiency relationship of [1,2,4]triazol-3-ylamines as novel nicotinamide isosteres that inhibit tankyrases.
Novartis Institutes For Biomedical Research
Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor.
Novartis Institutes For Biomedical Research
One-pot tandem Hurtley-retro-Claisen-cyclisation reactions in the synthesis of 3-substituted analogues of 5-aminoisoquinolin-1-one (5-AIQ), a water-soluble inhibitor of PARPs.
University of Bath
Discovery of novel benzo[b][1,4]oxazin-3(4H)-ones as poly(ADP-ribose)polymerase inhibitors.
Takeda California
Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors.
Amgen
Fragment-based ligand design of novel potent inhibitors of tankyrases.
Nanyang Technological University
In silico identification of poly(ADP-ribose)polymerase-1 inhibitors and their chemosensitizing effects against cisplatin-resistant human gastric cancer cells.
Sungkyunkwan [Corrected] University
Design, synthesis and biological evaluation of novel imidazo[4,5-c]pyridinecarboxamide derivatives as PARP-1 inhibitors.
China Pharmaceutical University
Design, synthesis, and biological evaluation of a series of benzo[de][1,7]naphthyridin-7(8H)-ones bearing a functionalized longer chain appendage as novel PARP1 inhibitors.
Chinese Academy of Sciences
Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket.
Amgen
Synopsis of some recent tactical application of bioisosteres in drug design.
Bristol-Myers Squibb Pharmaceutical Research and Development
Discovery and SAR of orally efficacious tetrahydropyridopyridazinone PARP inhibitors for the treatment of cancer.
Abbott Laboratories
[1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding.
Novartis Institutes For Biomedical Research
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
Cephalon
Structural basis for the interaction between tankyrase-2 and a potent Wnt-signaling inhibitor.
Karolinska Institutet
Design and synthesis of poly ADP-ribose polymerase-1 inhibitors. 2. Biological evaluation of aza-5[H]-phenanthridin-6-ones as potent, aqueous-soluble compounds for the treatment of ischemic injuries.
Guilford Pharmaceuticals
The discovery and synthesis of novel adenosine substituted 2,3-dihydro-1H-isoindol-1-ones: potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).
Inotek Pharmaceuticals
Synthesis of substituted 5[H]phenanthridin-6-ones as potent poly(ADP-ribose)polymerase-1 (PARP1) inhibitors.
Guilford Pharmaceuticals
Synthesis and SAR optimization of quinazolin-4(3H)-ones as poly(ADP-ribose)polymerase-1 inhibitors.
St. John'S University
Discovery and structure-activity relationships of modified salicylanilides as cell permeable inhibitors of poly(ADP-ribose) glycohydrolase (PARG).
University of Arizona
5-Benzamidoisoquinolin-1-ones and 5-(κ-carboxyalkyl)isoquinolin-1-ones as isoform-selective inhibitors of poly(ADP-ribose) polymerase 2 (PARP-2).
University of Bath
Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer.
Cylene Pharmaceuticals
Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinic.
Johns Hopkins University Brain Science Institute
Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.
Irbm/Merck Research Laboratories
Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor.
Abbott Laboratories
Synthesis and evaluation of tricyclic derivatives containing a non-aromatic amide as inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Jeil Pharmaceutical
Discovery and SAR of substituted 3-oxoisoindoline-4-carboxamides as potent inhibitors of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.
Abbott Laboratories
Identification and SAR of novel pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).
Irbm/Merck Research Laboratories
Development of substituted 6-[4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl]-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells.
Merck Research Laboratories
Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Irbm-Merck Research Laboratories Rome
Synthesis and biological evaluation of substituted 2-phenyl-2H-indazole-7-carboxamides as potent poly(ADP-ribose) polymerase (PARP) inhibitors.
Irbm-Merck Research Laboratories Rome
Synthesis of isoquinolinone-based tetracycles as poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors.
Sookmyung Women'S University
Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents.
Abbott Laboratories
Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Abbott Laboratories
Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase-1 inhibitors.
Irbm-Merck Research Laboratories Rome
Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors.
Irbm-Merck Research Laboratories Rome
Structural basis for inhibitor specificity in human poly(ADP-ribose) polymerase-3.
Institutet
New poly(ADP-ribose) polymerase-1 inhibitors with antioxidant activity based on 4-carboxamidobenzimidazole-2-ylpyrroline and -tetrahydropyridine nitroxides and their precursors.
University of Pecs
Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors.
Huazhong University of Science and Technology
Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.
University of Bath
Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent.
Abbott Laboratories
Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.
University of Cambridge
NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family.
Johann Wolfgang Goethe University
Indirubin derivatives as bifunctional molecules inducing DNA damage and targeting PARP for the treatment of cancer.
China Pharmaceutical University
Exploring the structural-activity relationship of hexahydropyrazino[1,2-d]pyrido[3,2-b][1,4]oxazine derivatives as potent and orally-bioavailable PARP7 inhibitors.
Guizhou University
Identification of [1,2,4]Triazolo[4,3-a]pyrazine PARP1 inhibitors with overcome acquired resistance activities.
Shanghai Jiao Tong University
Discovery of a novel dual-target inhibitor of CDK12 and PARP1 that induces synthetic lethality for treatment of triple-negative breast cancer.
Southwest Jiaotong University
Quinazolines annelated at the N(3)-C(4) bond: Synthesis and biological activity.
Ural Federal University
Re-Evaluating PIN1 as a Therapeutic Target in Oncology Using Neutral Inhibitors and PROTACs.
Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd.
Dual-target inhibitors of colchicine binding site for cancer treatment.
Henan University
Poly (ADP-ribose) polymerase (PARP) inhibitors as anticancer agents: An outlook on clinical progress, synthetic strategies, biological activity, and structure-activity relationship.
Acharya & BM Reddy College of Pharmacy
Leveraging a rationally designed veliparib-based anilide eliciting anti-leukemic effects for the design of pH-responsive polymer nanoformulation.
Taipei Medical University
Discovery of tricyclic PARP7 inhibitors with high potency, selectivity, and oral bioavailability.
Hubei Polytechnic University
Discovery of Highly Selective PARP7 Inhibitors with a Novel Scaffold for Cancer Immunotherapy.
China Pharmaceutical University
Small molecule targeted therapies for endometrial cancer: progress, challenges, and opportunities.
Yixing People's Hospital Yixing
Design and synthesis of the first PARP-1 and proteasome dual inhibitors to treat breast cancer.
Sichuan University
Targeting Myeloperoxidase Ameliorates Gouty Arthritis: A Virtual Screening Success Story.
University of Sao Paulo
Pyrrole-containing hybrids as potential anticancer agents: An insight into current developments and structure-activity relationships.
Jiangxi Science & Technology Normal University
High affinity and low PARP-trapping benzimidazole derivatives as a potential warhead for PARP1 degraders.
University of South China
Rational Design of PARP1/c-Met Dual Inhibitors for Overcoming PARP1 Inhibitor Resistance Induced by c-Met Overexpression.
China Pharmaceutical University
Design, Synthesis, and Structure-Activity Relationship of Novel Pyridazinone-Based PARP7/HDACs Dual Inhibitors for Elucidating the Relationship between Antitumor Immunity and HDACs Inhibition.
Hangzhou Normal University
Discovery and Proof of Concept of Potent Dual Polθ/PARP Inhibitors for Efficient Treatment of Homologous Recombination-Deficient Tumors.
China Pharmaceutical University
Advancements in dual-target inhibitors of PI3K for tumor therapy: Clinical progress, development strategies, prospects.
Sichuan University
Dual target PARP1/EZH2 inhibitors inducing excessive autophagy and producing synthetic lethality for triple-negative breast cancer therapy.
China Pharmaceutical University
Rational design of conformationally restricted quinazolinone inhibitors of poly(ADP-ribose)polymerase.
Astellas Pharma
New Horizons of Synthetic Lethality in Cancer: Current Development and Future Perspectives.
University of Bologna
Design, synthesis and biological evaluation of matrine contains benzimidazole derivatives as dual TOPOI and PARP inhibitors for cancer therapy.
Guangxi University
Synthesis and clinical application of small-molecule drugs approved to treat prostatic cancer.
Zhengzhou Normal University
Advances in Development of Selective Antitumor Inhibitors That Target PARP-1.
Shandong University
Discovery of Quinazoline-2,4(1
Chinese Academy of Medical Sciences and Peking Union Medical College
Expanding the Role of Boron in New Drug Chemotypes: Properties, Chemistry, Pharmaceutical Potential of Hemiboronic Naphthoids.
University of Alberta
An overview of compound properties, multiparameter optimization, and computational drug design methods for PARP-1 inhibitor drugs.
Niper Guwahati
Design, synthesis, biological evaluation and molecular docking study of novel urea-based benzamide derivatives as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors.
Sun Yat-Sen University
Discovery of novel benzamide derivatives bearing benzamidophenyl and phenylacetamidophenyl scaffolds as potential antitumor agents via targeting PARP-1.
Sun Yat-Sen University
Design and synthesis of novel chloropyridazine hybrids as promising anticancer agents acting by apoptosis induction and PARP-1 inhibition through a molecular hybridization strategy.
Ain-Shams University
A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.
China Pharmaceutical University
Hypoxia-activated prodrugs of phenolic olaparib analogues for tumour-selective chemosensitisation.
University of Auckland
Discovery, Synthesis, and Evaluation of Novel Dual Inhibitors of a Vascular Endothelial Growth Factor Receptor and Poly(ADP-Ribose) Polymerase for BRCA Wild-Type Breast Cancer Therapy.
Sichuan University
Discovery of the Potent and Highly Selective PARP7 Inhibitor as a Novel Immunotherapeutic Agent for Tumors.
China Pharmaceutical University
Synthesis of Veliparib Prodrugs and Determination of Drug-Release-Dependent PARP-1 Inhibition.
University of Pittsburgh
An Update on Poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors: Opportunities and Challenges in Cancer Therapy.
Shanghai Institute of Materia Medica
Insights into the recent progress in the medicinal chemistry of pyranopyrimidine analogs.
Mansoura University
Discovery of a Dual Tubulin and Poly(ADP-Ribose) Polymerase-1 Inhibitor by Structure-Based Pharmacophore Modeling, Virtual Screening, Molecular Docking, and Biological Evaluation.
China Pharmaceutical University
Multi-therapies Based on PARP Inhibition: Potential Therapeutic Approaches for Cancer Treatment.
Shandong First Medical University and Shandong Academy of Medical Sciences
β-Lactams as promising anticancer agents: Molecular hybrids, structure activity relationships and potential targets.
Beijing University of Chinese Medicine
The ups and downs of Poly(ADP-ribose) Polymerase-1 inhibitors in cancer therapy-Current progress and future direction.
Central South University
Optimization of a Screening Hit toward M2912, an Oral Tankyrase Inhibitor with Antitumor Activity in Colorectal Cancer Models.
Merck
Fused-azepinones: Emerging scaffolds of medicinal importance.
National Institute of Pharmaceutical Education and Research (NIPER)
Small-Molecule Inhibitors Targeting the Canonical WNT Signaling Pathway for the Treatment of Cancer.
Ocean University of China
Small-Molecule Drug Discovery in Triple Negative Breast Cancer: Current Situation and Future Directions.
Sichuan University
Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development.
West China Hospital of Sichuan University
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.
Panjab University
Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy.
West China Hospital of Sichuan University
Selective degradation of PARP2 by PROTACs via recruiting DCAF16 for triple-negative breast cancer.
West China Hospital of Sichuan University
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.
China Pharmaceutical University
Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-
Astrazeneca
Synthesis and structure-activity relationships of novel pyrrolocarbazole lactam analogs as potent and cell-permeable inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Cephalon
Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.
Cephalon
Phthalazinones 2: Optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase.
Kudos Pharmaceuticals
Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy: Advances, challenges, and opportunities.
West China Hospital
Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer.
China Pharmaceutical University
4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors.
Fujisawa Pharmaceutical
Evaluation of amentoflavone metabolites on PARP-1 inhibition and the potentiation on anti-proliferative effects of carboplatin in A549 cells.
China Pharmaceutical University
Structure-based design, synthesis, and evaluation of inhibitors with high selectivity for PARP-1 over PARP-2.
Shenyang Pharmaceutical University
Recent advances in DDR (DNA damage response) inhibitors for cancer therapy.
Hubei Polytechnic University
Small-molecule inhibitors of breast cancer-related targets: Potential therapeutic agents for breast cancer.
Shandong First Medical University & Shandong Academy of Medical Sciences
Medicinal Chemistry Perspective on Targeting Mono-ADP-Ribosylating PARPs with Small Molecules.
University of Perugia
Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.
Affiliated Hospital of Guangdong Medical University
Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy.
Nanjing University
Potent 2,3-dihydrophthalazine-1,4-dione derivatives as dual inhibitors for mono-ADP-ribosyltransferases PARP10 and PARP15.
University of Perugia
Small-Molecule Inhibitors of Tankyrases as Prospective Therapeutics for Cancer.
University of South Australia
Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase.
Kudos Horsham
Design, synthesis and pharmacological evaluation of new PARP1 inhibitors by merging pharmacophores of olaparib and the natural product alantolactone.
Shanghai Jiao Tong University
Synthesis and biological evaluation of a tumor-selective degrader of PARP1.
West China Hospital of Sichuan University
Design, synthesis, and bioactivity study on Lissodendrins B derivatives as PARP1 inhibitor.
Ocean University of China
Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.
Qingdao University Medical College
Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities.
Central South University
Pyridazine as a privileged structure: An updated review on anticancer activity of pyridazine containing bioactive molecules.
Key Laboratory of Technology of Drug Preparation (Zhengzhou University)
Discovery of Potent and Novel Dual PARP/BRD4 Inhibitors for Efficient Treatment of Pancreatic Cancer.
China Pharmaceutical University
Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase.
Pfizer
Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP.
Huazhong University of Science and Technology
Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase.
Fujisawa Pharmaceutical
Discovery of Novel Apigenin-Piperazine Hybrids as Potent and Selective Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors for the Treatment of Cancer.
China Pharmaceutical University
Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors.
University of Newcastle
Design, synthesis and biological evaluation of novel molecules as potent PARP-1 inhibitors.
China Pharmaceutical University
Discovery of novel and potent PARP/PI3K dual inhibitors for the treatment of cancer.
China Pharmaceutical University
Design and synthesis of poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors. Part 3: In vitro evaluation of 1,3,4,5-tetrahydro-benzo[c][1,6]- and [c][1,7]-naphthyridin-6-ones.
Guilford Pharmaceuticals
Discovery of Novel Bromophenol-Thiosemicarbazone Hybrids as Potent Selective Inhibitors of Poly(ADP-ribose) Polymerase-1 (PARP-1) for Use in Cancer.
Chinese Academy of Sciences
Discovery of novel PARP/PI3K dual inhibitors with high efficiency against BRCA-proficient triple negative breast cancer.
China Pharmaceutical University
Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure.
Pfizer
Substituted uracil derivatives as potent inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Bayer
Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers.
West China Hospital of Sichuan University
Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development.
TBA
Identification of 2-substituted pyrrolo[1,2-b]pyridazine derivatives as new PARP-1 inhibitors.
Central South University
Discovery of isoquinolinone and naphthyridinone-based inhibitors of poly(ADP-ribose) polymerase-1 (PARP1) as anticancer agents: Structure activity relationship and preclinical characterization.
Lupin
Modeling of poly(ADP-ribose)polymerase (PARP) inhibitors. Docking of ligands and quantitative structure-activity relationship analysis.
Università
Design, synthesis and anticancer activities of novel dual poly(ADP-ribose) polymerase-1/histone deacetylase-1 inhibitors.
Hefei University of Technology
Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor.
University of Oslo
Resistance-modifying agents. 9. Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase.
Newcastle University
Medicinal chemistry approaches of poly ADP-Ribose polymerase 1 (PARP1) inhibitors as anticancer agents - A recent update.
Nirma University
Discovery of Stereospecific PARP-1 Inhibitor Isoindolinone NMS-P515.
Nerviano Medical Sciences
Novel tricyclic poly (ADP-ribose) polymerase-1/2 inhibitors with potent anticancer chemopotentiating activity: Design, synthesis and biological evaluation.
China Pharmaceutical University
Design, synthesis and biological evaluation of novel 5-fluoro-1H-benzimidazole-4-carboxamide derivatives as potent PARP-1 inhibitors.
China Pharmaceutical University
Discovery of naphthacemycins as a novel class of PARP1 inhibitors.
North China Pharmaceutical Group
Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy.
TBA
Discovery of novel functionalized 1,2,4-triazoles as PARP-1 inhibitors in breast cancer: Design, synthesis and antitumor activity evaluation.
Suez Canal University
Synthesis and biological activity of structurally diverse phthalazine derivatives: A systematic review.
Y. B. Chavan College of Pharmacy
Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Newcastle University
Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer.
Japanese Foundation For Cancer Research
Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective Tankyrase Inhibitor Modulating Wnt Pathway Activity.
Merck Healthcare
Rational Design of Cell-Active Inhibitors of PARP10.
Oregon Health and Science University
Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering.
Astrazeneca
Synthesis and Evaluation of a Radioiodinated Tracer with Specificity for Poly(ADP-ribose) Polymerase-1 (PARP-1) in Vivo.
University of Glasgow
Design and Synthesis of Poly(ADP-ribose) Polymerase Inhibitors: Impact of Adenosine Pocket-Binding Motif Appendage to the 3-Oxo-2,3-dihydrobenzofuran-7-carboxamide on Potency and Selectivity.
St. John'S University
4-(Phenoxy) and 4-(benzyloxy)benzamides as potent and selective inhibitors of mono-ADP-ribosyltransferase PARP10/ARTD10.
University of Oulu
Targeting Wnt-driven cancers: Discovery of novel tankyrase inhibitors.
University of Perugia
Cell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides.
University of Manchester
Design and synthesis of 2-(4,5,6,7-tetrahydrothienopyridin-2-yl)-benzoimidazole carboxamides as novel orally efficacious Poly(ADP-ribose)polymerase (PARP) inhibitors.
Chinese Academy of Sciences
Identification by Inverse Virtual Screening of magnolol-based scaffold as new tankyrase-2 inhibitors.
University of Salerno
Design, synthesis and anticancer activities evaluation of novel 5H-dibenzo[b,e]azepine-6,11-dione derivatives containing 1,3,4-oxadiazole units.
China Medical University
Examination of Diazaspiro Cores as Piperazine Bioisosteres in the Olaparib Framework Shows Reduced DNA Damage and Cytotoxicity.
University of Pennsylvania
Design, synthesis and biological evaluation of 4-amidobenzimidazole acridine derivatives as dual PARP and Topo inhibitors for cancer therapy.
Tsinghua University
Discovery, mechanism and metabolism studies of 2,3-difluorophenyl-linker-containing PARP1 inhibitors with enhanced in vivo efficacy for cancer therapy.
East China University of Science and Technology
Design, synthesis and evaluation of potent and selective inhibitors of mono-(ADP-ribosyl)transferases PARP10 and PARP14.
Mcdaniel College
Discovery of novel quinazoline-2,4(1H,3H)-dione derivatives as potent PARP-2 selective inhibitors.
Peking Union Medical College
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.
Tsinghua University
Lead Discovery of Dual G-Quadruplex Stabilizers and Poly(ADP-ribose) Polymerases (PARPs) Inhibitors: A New Avenue in Anticancer Treatment.
Regina Elena National Cancer Institute
Discovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach.
Leibniz-Forschungsinstitut F�R Molekulare Pharmakologie (Fmp)
Identification of low micromolar dual inhibitors for aldose reductase (ALR2) and poly (ADP-ribose) polymerase (PARP-1) using structure based design approach.
Punjabi University
Discovery of 2-substituted 1H-benzo[d]immidazole-4-carboxamide derivatives as novel poly(ADP-ribose)polymerase-1 inhibitors with in vivo anti-tumor activity.
Peking Union Medical College
Design and synthesis of potent inhibitors of the mono(ADP-ribosyl)transferase, PARP14.
Mcdaniel College
Inhibitors of guanosine monophosphate synthetase as therapeutic agents
University of Southern California
Pyrrolopyrimidine derivative and use thereof
Wuhan Humanwell Innovative Drug Research And Development Center
HETEROBIVALENT AND HOMOBIVALENT AGENTS TARGETING FIBROBLAST ACTIVATION PROTEIN ALPHA AND/OR PROSTATE-SPECIFIC MEMBRANE ANTIGEN
The Johns Hopkins University
COMPOUNDS AND RADIOLIGANDS FOR TARGETING NEUROTENSIN RECEPTOR AND USES THEREOF
Full-Life Technologies HK
CYCLIN-DEPENDENT KINASE INHIBITING COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS
G1 Therapeutics
2-amino-N-(arylsulfinyl)-acetamide compounds as inhibitors of bacterial aminoacyl-tRNA synthetase
Oxford Drug Design
Solid forms of a plasma kallikrein inhibitor and salts thereof
Kalvista Pharmaceuticals
Mitogen-activated protein kinase inhibitors, methods of making, and methods of use thereof
Washington University
Sulfonimidoylpurinone compounds and methods of treatment using the same
Hoffmann-La Roche
Tetrahydroquinoline-based bromodomain inhibitors
St. Jude Children'S Research Hospital
Substituted thiohydantoin derivatives as androgen receptor antagonists
Janssen Pharmaceutica
Screening of drugs by FRET analysis identifies inhibitors of SARS-CoV 3CL protease.
National Taiwan University
Oxamic acid analogues as LDH-C4-specific competitive inhibitors.
Instituto Politécnico Nacional
Structure-Based Screening of Uncharted Chemical Space for Atypical Adenosine Receptor Agonists
Uppsala University
Beta carboline derivatives useful in the treatment of proliferative disorders
Facultes Universitaires Notre Dame De La Paix
Synthesis, in vitro evaluation and molecular docking studies of biscoumarin thiourea as a new inhibitor of a-glucosidases.
Universiti Teknologi Mara
Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof
Albany Molecular Research
Bivalent diazo bicyclic Smac mimetics and the uses thereof
The Regents of The University of Michigan
Discovery of HIV-1 integrase inhibitors: pharmacophore mapping, virtual screening, molecular docking, synthesis, and biological evaluation.
Nirma University
Solution-phase parallel synthesis of carbamates as gamma-secretase inhibitors.
Schering-Plough Research Institute
Design, synthesis, and biological evaluation of new 3-hydroxy-2-oxo-3-trifluoromethylindole as potential HIV-1 reverse transcriptase inhibitors
Instituto De Tecnologia Em Fa��Rmacos
Probing the active site of the deoxynucleotide N-hydrolase Rcl encoded by the rat gene c6orf108.
Institut Pasteur
Discovery of PDK1 kinase inhibitors with a novel mechanism of action by ultrahigh throughput screening.
Merck Research Laboratories
Antidepressant-like activity and modulation of brain monoaminergic transmission by blockade of anandamide hydrolysis.
Mcgill University
Preclinical profile of ciclesonide, a novel corticosteroid for the treatment of asthma.
Imperial College
The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways.
Institut De Recherches Servier
[125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.
Novartis Pharma
Characterization of binding sites of a new neurotensin receptor antagonist, [3H]SR 142948A, in the rat brain.
Hospital Saint-Antoine
Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine.
University of Toronto
Characterization of [3H]quinpirole binding to D2-like dopamine receptors in rat brain.
Dupont Pharmaceuticals
Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors.
Abbott Laboratories
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.
National Institutes of Health
Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
Enanta Pharmaceuticals