Synthesis and biological study of 2-amino-4-aryl-5-chloropyrimidine analogues as inhibitors of VEGFR-2 and cyclin dependent kinase 1 (CDK1)

被引：15
作者：
Huang, Shenlin
Li, Ronghua
Connolly, Peter J.
Emanuel, Stuart
Fuentes-Pesquera, Angel
Adams, Mary
Gruninger, Robert H.
Seraj, Jabed
Middleton, Steven A.
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 / 08期
关键词：
CDK1; VEGFR-2; 2-amino-4-aryl-5-chloropyrimidine; ENDOTHELIAL GROWTH-FACTOR; PYRIMIDINE PAP DERIVATIVES; CYCLIN-DEPENDENT KINASE; SELECTIVE INHIBITORS; CLINICAL DEVELOPMENT; CANCER; ANGIOGENESIS; TARGETS; THERAPY; POTENT;
D O I：
10.1016/j.bmcl.2007.01.086
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The series of 2-amiiio-4-aryl-5-chloropyrimidines was discovered to be potent for both VEGFR-2 and CDK1. Described here are the chemistry for analogue synthesis, SAR study, and its kinase selectivity prolifing. The full rat PK data and in vivo efficacy study are also included. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2179 / 2183
页数：5
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