Kiselyov, Alexander S.; Milligan, Daniel; Ouyang, Xiaohu published the artcile< Novel inhibitors of VEGF receptors-1 and -2 based on azole-5-carboxamide templates>, Synthetic Route of 112-63-0, 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. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Synthetic Route of 112-63-0.
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