Quality Control of 2,6-Difluorobenzoic acid. Waaler, J; Leenders, RGG; Sowa, ST; Brinch, SA; Lycke, M; Nieczypor, P; Aertssen, S; Murthy, S; Galera-Prat, A; Damen, E; Wegert, A; Nazare, M; Lehtio, L; Krauss, S in [Waaler, Jo; Brinch, Shoshy Alam; Lycke, Max; Krauss, Stefan] Univ Oslo, Inst Basic Med Sci, Ctr Excellence, Hybrid Technol Hub, N-0317 Oslo, Norway; [Waaler, Jo; Brinch, Shoshy Alam; Lycke, Max; Krauss, Stefan] Oslo Univ Hosp, Dept Immunol & Transfus Med, N-0424 Oslo, Norway; [Leenders, Ruben G. G.; Nieczypor, Piotr; Aertssen, Sjoerd; Damen, Eddy; Wegert, Anita] Mercachem BV, NL-6546 BB Nijmegen, Netherlands; [Sowa, Sven T.; Murthy, Sudarshan; Galera-Prat, Albert; Lehtio, Lari] Univ Oulu, Bioctr Oulu, Fac Biochem & Mol Med, Oulu 90014, Finland; [Nazare, Marc] Campus Berlin Buch, Leibniz Forschungsinst Mol Pharmakol, Med Chem, D-13125 Berlin, Germany published Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor in 2020, Cited 40. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2.
Tankyrases 1 and 2 are central biotargets in the WNT/beta-catenin signaling and Hippo signaling pathways. We have previously developed tankyrase inhibitors bearing a 1,2,4-triazole moiety and binding predominantly to the adenosine binding site of the tankyrase catalytic domain. Here we describe a systematic structure-guided lead optimization approach of these tankyrase inhibitors. The central 1,2,4-triazole template and trans-cyclobutyl linker of the lead compound 1 were left unchanged, while side-group East, West, and South moieties were altered by introducing different building blocks defined as point mutations. The systematic study provided a novel series of compounds reaching picomolar IC50 inhibition in WNT/beta-catenin signaling cellular reporter assay. The novel optimized lead 13 resolves previous atropisomerism, solubility, and Caco-2 efflux liabilities. 13 shows a favorable ADME profile, including improved Caco-2 permeability and oral bioavailability in mice, and exhibits antiproliferative efficacy in the colon cancer cell line COLO 320DM in vitro.
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