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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.

Universit£

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

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

Chinese Academy of Medical Sciences and 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.

Chinese Academy of Medical Sciences & 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.

Chinese Academy of Medical Sciences & Peking Union Medical College

Synthesis and carbonic anhydrase inhibitory properties of novel 1,4-dihydropyrimidinone substituted diarylureas.

Sakarya University

Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.

Stony Brook University

Characterization of a 5-hydroxytryptamine receptor in mouse neuroblastoma N18TG2 cells.

University of Pennsylvania

Selective activation of inhibitory G-protein alpha-subunits by partial agonists of the human 5-HT1A receptor.

Medical University of South Carolina

Discovery of potent inhibitors of interleukin-2 inducible T-cell kinase (ITK) through structure-based drug design.

Boehringer Ingelheim Pharmaceuticals