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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

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

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

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

Development of novel dual binders as potent, selective, and orally bioavailable tankyrase inhibitors.

Amgen

Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.

Amgen

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, 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

Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket.

Amgen

Structural basis of selective inhibition of human tankyrases.

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.

Novartis Institutes For Biomedical Research

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

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

Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).

Irbm-Merck Research Laboratories Rome

Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase-1 inhibitors.

Irbm-Merck Research Laboratories Rome

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

YCH1899, a Highly Effective Phthalazin-1(2

Shanghai Institute of Materia Medica

Discovery of novel benzamide derivatives bearing benzamidophenyl and phenylacetamidophenyl scaffolds as potential antitumor agents via targeting PARP-1.

Sun Yat-Sen University

A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.

China Pharmaceutical University

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

[1,2,4]Triazolo[3,4-

University of Oulu

Discovery of the Potent and Highly Selective PARP7 Inhibitor as a Novel Immunotherapeutic Agent for Tumors.

China Pharmaceutical University

An Update on Poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors: Opportunities and Challenges in Cancer Therapy.

Shanghai Institute of Materia Medica

Multi-therapies Based on PARP Inhibition: Potential Therapeutic Approaches for Cancer Treatment.

Shandong First Medical University and Shandong Academy of Medical Sciences

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

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

Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy: Advances, challenges, and opportunities.

West China Hospital

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

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

Rational design of selective inhibitors of PARP4.

Initial Therapeutics

Analogs of TIQ-A as inhibitors of human mono-ADP-ribosylating PARPs.

University of Oulu

Discovery of Potent and Novel Dual PARP/BRD4 Inhibitors for Efficient Treatment of Pancreatic Cancer.

China Pharmaceutical University

Discovery of Quinazoline-2,4(1

Peking Union Medical College

Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II.

Symeres

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

Discovery of novel and potent PARP/PI3K dual inhibitors for the treatment of cancer.

China Pharmaceutical University

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

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

Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor.

University of Oslo

From PARP1 to TNKS2 Inhibition: A Structure-Based Approach.

University of Naples

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

Discovery of Novel Spiroindoline Derivatives as Selective Tankyrase Inhibitors.

Riken

Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy.

TBA

Synthesis and biological activity of structurally diverse phthalazine derivatives: A systematic review.

Y. B. Chavan College of Pharmacy

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

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

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

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

Discovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach.

Leibniz-Forschungsinstitut F�R Molekulare Pharmakologie (Fmp)

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

HETEROBIVALENT AND HOMOBIVALENT AGENTS TARGETING FIBROBLAST ACTIVATION PROTEIN ALPHA AND/OR PROSTATE-SPECIFIC MEMBRANE ANTIGEN

The Johns Hopkins University

NEW PYRIDO DIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAM

Hoffmann-La Roche

MODULATORS OF SORTILIN ACTIVITY

Insusense

Inhibtors of Raf kinases

Kinnate Biopharma

2-amino-N-(arylsulfinyl)-acetamide compounds as inhibitors of bacterial aminoacyl-tRNA synthetase

Oxford Drug Design

Substituted pyridines as PARP1 inhibitors

Xinthera

Inhibitors of VAP-1

Acucela

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

Tetrahydroquinoline-based bromodomain inhibitors

St. Jude Children'S Research Hospital

1,8-naphthyridinone compounds and uses thereof

Nuvation Bio

Isoquinolin-3-yl carboxamides and preparation and use thereof

Samumed

Pyrido[2,3-d]pyrimidin-4-one compounds as tankyrase inhibitors

Eli Lilly

Compounds and methods for kinase modulation, and indications therefor

Plexxikon

Kinase inhibitors

University of California

Quinoline derivatives as PDE10A enzyme inhibitors

H. Lundbeck

Morpholine derivative

Shanghai Pharmaceuticals Holding

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

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 [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