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

被引：22

作者：

Hughes, Terry V. ^{[1
]}

Emanuel, Stuart L. ^{[1
]}

O'Grady, Harold R. ^{[1
]}

Connolly, Peter J. ^{[1
]}

Rugg, Catherine ^{[1
]}

Fuentes-Pesquera, Angel R. ^{[1
]}

Karnachi, Prabha ^{[1
]}

Alexander, Richard ^{[1
]}

Middleton, Steven A. ^{[1
]}

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev LLC, Raritan, NJ 08869 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 18期

关键词：

cancer; Aurora-A; Aurora-B; Aurora-C; kinase; vascular endothelial growth factor receptor 2; VEGF-R2; kinase inhibition; isoindolinone; 2,3-dihydro-isoindol-1-ones;

D O I：

10.1016/j.bmcl.2008.07.090

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of 7-[1H-indol-2-yl]-2,3-dihydro-isoindol-1-ones designed to be inhibitors of VEGF-R2 kinase was synthesized and found to potently inhibit VEGF-R2 and Aurora-A kinases. The structure-based design, synthesis, and initial SAR of the series are discussed. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：5130 / 5133

页数：4

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