Identification of selective inhibitors of cyclin dependent kinase 4

被引:52
作者
Carini, DJ [1 ]
Kaltenbach, RF
Liu, J
Benfield, PA
Boylan, J
Boisclair, M
Brizuela, L
Burton, CR
Cox, S
Grafstrom, R
Harrison, BA
Harrison, K
Akamike, E
Markwalder, JA
Nakano, Y
Seitz, SP
Sharp, DM
Trainor, GL
Sielecki, TM
机构
[1] Dupont Merck Pharmaceut Co, Wilmington, DE 19880 USA
[2] Mitotix Inc, Cambridge, MA USA
关键词
D O I
10.1016/S0960-894X(01)00416-4
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
A new structural type of kinase inhibitor. containing a benzocarbazole nucleus, has been identified. Members of the series are selective for inhibition of the cyclin dependent kinase family of enzymes. Although the cdks are highly homologous, representatives of the series showed intra-cdk selectivities, especially for cdk4. SAR studies elucidated the important features of the molecules for inhibition. (C) 2001 DuPont Pharmaceuticals Company. Published by Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2209 / 2211
页数:3
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