I found the field of Pharmacology & Pharmacy very interesting. Saw the article Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor published in 2020. Application In Synthesis of 2,6-Difluorobenzoic acid, Reprint Addresses Waaler, J (corresponding author), Univ Oslo, Inst Basic Med Sci, Ctr Excellence, Hybrid Technol Hub, N-0317 Oslo, Norway.; Waaler, J (corresponding author), Oslo Univ Hosp, Dept Immunol & Transfus Med, N-0424 Oslo, Norway.. The CAS is 385-00-2. Through research, I have a further understanding and discovery of 2,6-Difluorobenzoic acid
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.
Application In Synthesis of 2,6-Difluorobenzoic acid. Bye, fridends, I hope you can learn more about C7H4F2O2, If you have any questions, you can browse other blog as well. See you lster.
Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com