Synthesis of C2 alkynylated purines, a new family of potent inhibitors of cyclin-dependent kinases

被引:50
作者
Legraverend, M
Ludwig, O
Bisagni, E
Leclerc, S
Meijer, L
机构
[1] Ctr Univ Orsay, Inst Curie, UMR 176 CNRS, F-91405 Orsay, France
[2] CNRS, Biol Stn, F-29682 Roscoff, France
关键词
D O I
10.1016/S0960-894X(98)00097-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of a new family of inhibitors of the cell cycle regulating cyclin-dependent kinases (CDK's) is reported. These compounds, related to the purines olomoucine and roscovitine, are characterised by the presence of alkynylated side chains at C2. They inhibit CDK's with IC50's in the 200 nM range. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:793 / 798
页数:6
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