7-[1H-Indol-2-yl]-2, 3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: Design, synthesis, and biological activity

…, PJ Connolly, C Rugg, AR Fuentes-Pesquera…

Index: Hughes, Terry V.; Emanuel, Stuart L.; O'Grady, Harold R.; Connolly, Peter J.; Rugg, Catherine; Fuentes-Pesquera, Angel R.; Karnachi, Prabha; Alexander, Richard; Middleton, Steven A. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 18 p. 5130 - 5133

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Citation Number: 16

Abstract

The design of a new kinase inhibitor scaffold 1 based on known VEGF-R2 kinase inhibitors is described. The series designed to be inhibitors of VEGF-R2 kinase were synthesized and found to potently inhibit VEGF-R2 and Aurora-A kinases. The structure-based design, synthesis, initial SAR, and in vivo efficacy of the series are discussed. ... Vascular endothelial growth factor (VEGF) is an important regulator of vascular growth and permeability. Overexpression of ...