ArticleACS medicinal chemistry letters2013
Design and Discovery of 2-Arylquinazolin-4-ones as Potent and Selective Inhibitors of Tankyrases.
Article in ACS medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 41 citations in OpenAlex.
- Discovery of Quinazolone Pyridiniums as Potential Broad-Spectrum Antibacterial Agents.Molecules (Basel, Switzerland) · 2025Article
- Combining pharmacophore models derived from DNA-encoded chemical libraries with structure-based exploration to predict Tankyrase 1 inhibitors.European journal of medicinal chemistry · 2023Article
- Discovery of Novel Inhibitor for WNT/β-Catenin Pathway by Tankyrase 1/2 Structure-Based Virtual Screening.Molecules (Basel, Switzerland) · 2020Article
- 3D-QSAR, Docking, ADME/Tox studies on Flavone analogs reveal anticancer activity through Tankyrase inhibition.Scientific reports · 2019Article
- Bismuth-Catalyzed Synthesis of 2-Substituted Quinazolinones.Tetrahedron letters · 2018Article
- Identification of Novel Target for Osteosarcoma by Network Analysis.Medical science monitor : international medical journal of experimental and clinical research · 2018Article
- 2-Phenylquinazolinones as dual-activity tankyrase-kinase inhibitors.Scientific reports · 2018Article
- Regulation of Wnt/β-catenin signalling by tankyrase-dependent poly(ADP-ribosyl)ation and scaffolding.British journal of pharmacology · 2017Review
- Fragment-Based Drug Design of Novel Pyranopyridones as Cell Active and Orally Bioavailable Tankyrase Inhibitors.ACS medicinal chemistry letters · 2015Article
- Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivo pharmacology.ACS medicinal chemistry letters · 2015Article
- Small-molecule inhibitors of Wnt signaling pathway: towards novel anticancer therapeutics.Future medicinal chemistry · 2015Review
- Tankyrases: structure, function and therapeutic implications in cancer.Current pharmaceutical design · 2014Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Tankyrases (TNKSs) are poly(ADP-ribose)polymerases (PARPs) that are overexpressed in several clinical cancers. They regulate elongation of telomeres, regulate the Wnt system, and are essential for the function of the mitotic spindle. A set of 2-arylquinazolin-4-ones has been designed and identified as potent and selective TNKS inhibitors, some being more potent and selective than the lead inhibitor XAV939, with IC50 = 3 nM vs. TNKS-2. Methyl was preferred at the 8-position and modest bulk at the 4-position of the 2-phenyl group; electronic effects and H-bonding were irrelevant, but charge in the 4'-substituent must be avoided. Molecular modeling facilitated initial design of the compounds and rationalization of the SAR of binding into the nicotinamide-binding site of the target enzymes. These compounds have potential for further development into anticancer drugs.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.