Kiselyov, Alexander S. published the artcileNovel inhibitors of VEGF receptors-1 and -2 based on azole-5-carboxamide templates, Quality Control of 5805-53-8, the main research area is inhibitor VEGF receptor azole carboxamide preparation SAR.
We have developed a series of novel potent 1-(2-(pyridin-4-yl)ethyl)-1H-azole-5-carboxamides active against kinases VEGFR-2 and -1. Both specific and dual ATP-competitive inhibitors of VEGFR-2 were identified. Kinase selectivity could be controlled by varying the 5-carboxamide substituent at the azole ring. The most specific mols. displayed >10-fold selectivity for VEGFR-2 over VEGFR-1. Compound activities in vitro and in cell-based assays (IC50 < 100 nM) were similar to those of reported clin. and development candidates, including PTK787 (Vatalanibtrade) and ZD6474 (Vandetanib). High permeability of active compounds across the Caco-2 cell monolayer (>40×10-5 cm/min) is indicative of their potential for intestinal absorption upon oral administration.
Bioorganic & Medicinal Chemistry Letters published new progress about Homo sapiens. 5805-53-8 belongs to class imidazoles-derivatives, name is Methyl 1H-benzo[d]imidazole-2-carboxylate, and the molecular formula is C9H8N2O2, Quality Control of 5805-53-8.
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem