4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: Synthesis and biological evaluation

被引：42

作者：

Hughes, Terry V.

Emanuel, Stuart L.

Beck, Amanda K.

Wetter, Steven K.

Connolly, Peter J.

Karnachi, Prabha

Reuman, Michael

Seraj, Jabed

Fuentes-Pesquera, Angel R.

Gruninger, Robert H.

Middleton, Steven A.

Lin, Ronghui

Davis, Jeremy M.

Moffat, David F. C.

机构：

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

[2] UCB Pharma, Slough SL1 4EN, Berks, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 12期

关键词：

VEGF-R2; kinase; KDR; cancer; angiogenesis; kinase inhibitor; 2-aminopyrimidines;

D O I：

10.1016/j.bmcl.2007.04.021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of 4-aryl-5-cyano-2-aminopyrimidines were synthesized and found to have potent VEGF-R2 kinase inhibitory activity. Structure-activity relationships were investigated and compound 14a was shown to be efficacious in a mouse model of corneal neovascularization. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：3266 / 3270

页数：5

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