ortho-Substituted azoles as selective and dual inhibitors of VEGF receptors 1 and 2

…, EL Piatnitski, AV Samet, VP Kisliy, VV Semenov

Index: Kiselyov, Alexander S.; Piatnitski, Evgueni L.; Samet, Alexander V.; Kisliy, Victor P.; Semenov, Victor V. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 5 p. 1369 - 1375

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Citation Number: 17

Abstract

We have developed a series of novel potent ortho-substituted azole derivatives active against kinases VEGFR-1 and VEGFR-2. Both specific and dual ATP-competitive inhibitors of VEGFR-2 were identified. Kinase activity and selectivity could be controlled by varying the arylamido substituents at the azole ring. The most specific molecule (17) displayed> 10-fold selectivity for VEGFR-2 over VEGFR-1. Compound activities in enzymatic and cell-based ...