Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: Identification and optimisation of substituted 4,6-bis anilino pyrimidines

被引:80
作者
Beattie, JF [1 ]
Breault, GA [1 ]
Ellston, RPA [1 ]
Green, S [1 ]
Jewsbury, PJ [1 ]
Midgley, CJ [1 ]
Naven, RT [1 ]
Minshull, CA [1 ]
Pauptit, RA [1 ]
Tucker, JA [1 ]
Pease, JE [1 ]
机构
[1] AstraZeneca, Macclesfield SK10 4TG, Cheshire, England
关键词
D O I
10.1016/S0960-894X(03)00202-6
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Using a high-throughput screening campaign, we identified the 4,6-bis anilino pyrimidines as inhibitors of the cyclin-dependent kinase. CDK4. Herein we describe the further chemical modification and use of X-ray crystallography to develop potent and selective in vitro inhibitors of CDK4. (C) 2003 Elsevier Ltd. All rights reserved.
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收藏
页码:2955 / 2960
页数:6
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