Computed Properties of C7H4F2O2. Recently I am researching about SELECTIVE INHIBITORS; DISCOVERY; CATENIN; POTENT; GROWTH; CELLS; ASSAY; SITE, Saw an article supported by the Research Council of NorwayResearch Council of Norway [262613, 267639, 296226]; SouthEastern Norway Regional Health Authority [16/005289, 15/00779-2, 2015012, 2019090]; Norwegian Cancer SocietyNorwegian Cancer Society [5803958]; Jane and Aatos Erkko Foundation; Academy of FinlandAcademy of FinlandEuropean Commission [287063, 294085, 319299]; Sigrid Juselius FoundationSigrid Juselius Foundation. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: 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. 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.
Computed Properties of C7H4F2O2. About 2,6-Difluorobenzoic acid, If you have any questions, you can contact 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 or concate me.
Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com