Inhibitors of VEGF receptors-1 and-2 based on the 2-((pyridin-4-yl) ethyl) pyridine template

AS Kiselyov, M Semenova, VV Semenov…

Index: Kiselyov, Alexander S.; Semenova, Marina; Semenov, Victor V.; Milligan, Daniel Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 7 p. 1913 - 1919

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Citation Number: 16

Abstract

We have developed a series of novel potent ((pyridin-4-yl) ethyl) pyridine derivatives active against kinases VEGFR-1 and-2. Both specific and dual ATP-competitive inhibitors of VEGFR-2 were identified. Kinase selectivity could be controlled by varying the arylamino substituent at the 1, 3, 4-oxadiazole ring. The most specific molecules displayed> 10-fold selectivity for VEGFR-2 over VEGFR-1. Compound activities in vitro and in cell-based ...