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116 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
Structure-activity relationships of 2-arylquinazolin-4-ones as highly selective and potent inhibitors of the tankyrases.EBI
University Of Bath
Potential Use of Inhibitors of Tankyrases and PARP-1 as Treatment for Cancer and Other Diseases.EBI
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.EBI
Biomarin Pharmaceutical
Development and structural analysis of adenosine site binding tankyrase inhibitors.EBI
University Of Oulu
Selective inhibition of PARP10 using a chemical genetics strategy.EBI
Oregon Health & Science University
Identification of novel PARP-1 inhibitors: Drug design, synthesis and biological evaluation.EBI
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.EBI
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.EBI
Nerviano Medical Sciences
Discovery of potent and selective nonplanar tankyrase inhibiting nicotinamide mimics.EBI
University Of Oulu
Benzimidazole derivatives as potential dual inhibitors for PARP-1 and DHODH.EBI
University Of Malaya
Structure-based design, synthesis and evaluation in vitro of arylnaphthyridinones, arylpyridopyrimidinones and their tetrahydro derivatives as inhibitors of the tankyrases.EBI
University Of Bath
Tankyrase 1 Inhibitors with Drug-like Properties Identified by Screening a DNA-Encoded Chemical Library.EBI
Philochem
Niraparib: A Poly(ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination.EBI
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.EBI
Peking University
Towards small molecule inhibitors of mono-ADP-ribosyltransferases.EBI
Karolinska Institutet
Synthesis and biological evaluation of isoindoloisoquinolinone, pyroloisoquinolinone and benzoquinazolinone derivatives as poly(ADP-ribose) polymerase-1 inhibitors.EBI
Pondicherry University
Synthesis and biological evaluation of substituted 4-(thiophen-2-ylmethyl)-2H-phthalazin-1-ones as potent PARP-1 inhibitors.EBI
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.EBI
St. John'S University
Synthesis of isoquinolinone-based tricycles as novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors.EBI
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.EBI
Universit£
Nitric oxide (NO) releasing poly ADP-ribose polymerase 1 (PARP-1) inhibitors targeted to glutathione S-transferase P1-overexpressing cancer cells.EBI
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.EBI
Washington University Saint Louis
Evaluation and Structural Basis for the Inhibition of Tankyrases by PARP Inhibitors.EBI
University Of Oulu
7-Azaindole-1-carboxamides as a new class of PARP-1 inhibitors.EBI
Universit£
Novel PARP-1 inhibitors based on a 2-propanoyl-3H-quinazolin-4-one scaffold.EBI
R&D Sigma-Tau Industrie Farmaceutiche Riunite
Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.EBI
Amgen
Design and Discovery of 2-Arylquinazolin-4-ones as Potent and Selective Inhibitors of Tankyrases.EBI
University Of Bath
Chemical probes to study ADP-ribosylation: synthesis and biochemical evaluation of inhibitors of the human ADP-ribosyltransferase ARTD3/PARP3.EBI
Ume£
Identification of novel PARP-1 inhibitors by structure-based virtual screening.EBI
St. John'S University
Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity.EBI
University Of Oulu
Structure-efficiency relationship of [1,2,4]triazol-3-ylamines as novel nicotinamide isosteres that inhibit tankyrases.EBI
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.EBI
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.EBI
University Of Bath
Discovery of novel benzo[b][1,4]oxazin-3(4H)-ones as poly(ADP-ribose)polymerase inhibitors.EBI
Takeda California
Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors.EBI
Amgen
Fragment-based ligand design of novel potent inhibitors of tankyrases.EBI
Nanyang Technological University
In silico identification of poly(ADP-ribose)polymerase-1 inhibitors and their chemosensitizing effects against cisplatin-resistant human gastric cancer cells.EBI
Sungkyunkwan [Corrected] University
Design, synthesis and biological evaluation of novel imidazo[4,5-c]pyridinecarboxamide derivatives as PARP-1 inhibitors.EBI
China Pharmaceutical University
Screening and structural analysis of flavones inhibiting tankyrases.EBI
University Of Oulu
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.EBI
Chinese Academy Of Sciences
Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket.EBI
Amgen
Synopsis of some recent tactical application of bioisosteres in drug design.EBI
Bristol-Myers Squibb Pharmaceutical Research And Development
Discovery and SAR of orally efficacious tetrahydropyridopyridazinone PARP inhibitors for the treatment of cancer.EBI
Abbott Laboratories
Structural basis of selective inhibition of human tankyrases.EBI
Abo Akademi University
[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.EBI
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.EBI
Cephalon
Structural basis for the interaction between tankyrase-2 and a potent Wnt-signaling inhibitor.EBI
Karolinska Institutet
Novel poly(ADP-ribose) polymerase-1 inhibitors.EBI
Cephalon
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.EBI
Guilford Pharmaceuticals
Synthesis of substituted 5[H]phenanthridin-6-ones as potent poly(ADP-ribose)polymerase-1 (PARP1) inhibitors.EBI
Guilford Pharmaceuticals
Synthesis and SAR optimization of quinazolin-4(3H)-ones as poly(ADP-ribose)polymerase-1 inhibitors.EBI
St. John'S University
Novel poly(ADP-ribose) polymerase-1 inhibitors.EBI
Cephalon
Discovery and structure-activity relationships of modified salicylanilides as cell permeable inhibitors of poly(ADP-ribose) glycohydrolase (PARG).EBI
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).EBI
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.EBI
Cylene Pharmaceuticals
Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinic.EBI
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.EBI
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.EBI
Abbott Laboratories
Synthesis and evaluation of tricyclic derivatives containing a non-aromatic amide as inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).EBI
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.EBI
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).EBI
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.EBI
Merck Research Laboratories
Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).EBI
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.EBI
Irbm-Merck Research Laboratories Rome
Synthesis of isoquinolinone-based tetracycles as poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors.EBI
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.EBI
Abbott Laboratories
Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).EBI
Abbott Laboratories
Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase-1 inhibitors.EBI
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.EBI
Irbm-Merck Research Laboratories Rome
Structural basis for inhibitor specificity in human poly(ADP-ribose) polymerase-3.EBI
Institutet
Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors.EBI
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.EBI
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.EBI
Abbott Laboratories
Rational design of conformationally restricted quinazolinone inhibitors of poly(ADP-ribose)polymerase.EBI
Astellas Pharma
Synthesis and structure-activity relationships of novel pyrrolocarbazole lactam analogs as potent and cell-permeable inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).EBI
Cephalon
Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.EBI
Cephalon
Phthalazinones 2: Optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase.EBI
Kudos Pharmaceuticals
4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors.EBI
Fujisawa Pharmaceutical
Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase.EBI
Kudos Horsham
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.EBI
Pfizer
Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase.EBI
Fujisawa Pharmaceutical
Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors.EBI
University Of Newcastle
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.EBI
Guilford Pharmaceuticals
Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors.EBI
Pfizer
Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure.EBI
Pfizer
Substituted uracil derivatives as potent inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).EBI
Bayer
Modeling of poly(ADP-ribose)polymerase (PARP) inhibitors. Docking of ligands and quantitative structure-activity relationship analysis.EBI
Università
Resistance-modifying agents. 9. Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase.EBI
Newcastle University
Novel inhibitor of bacterial sphingomyelinase, SMY-540, developed based on three-dimensional structure analysis.BDB
Tokushima Bunri University
Polyphenol fatty acid esters as serine protease inhibitors: a quantum-chemical QSAR analysis.BDB
Slovak University Of Technology
Novel N-hydroxybenzamides incorporating 2-oxoindoline with unexpected potent histone deacetylase inhibitory effects and antitumor cytotoxicity.BDB
Hanoi University Of Pharmacy
Crystal structure of 3-hydroxybenzoate 6-hydroxylase uncovers lipid-assisted flavoprotein strategy for regioselective aromatic hydroxylation.BDB
Wageningen University
Expression and pharmacological characterization of the human D3 dopamine receptor.BDB
Neuroscience Research Centre
Characterization of a 5-hydroxytryptamine receptor in mouse neuroblastoma N18TG2 cells.BDB
University Of Pennsylvania
Melatonin receptors: localization, molecular pharmacology and physiological significance.BDB
Rowett Research Institute
Selective activation of inhibitory G-protein alpha-subunits by partial agonists of the human 5-HT1A receptor.BDB
Medical University Of South Carolina
Characterization of [3H]RX821002 binding to alpha-2 adrenergic receptor subtypes.BDB
University Of Nebraska
Dopamine D1 receptors: efficacy of full (dihydrexidine) vs. partial (SKF38393) agonists in primates vs. rodents.BDB
University Of North Carolina