Structure-based design of potent CDK1 inhibitors derived from olomoucine

被引:36
作者
Furet, P [1 ]
Zimmermann, J [1 ]
Capraro, HG [1 ]
Meyer, T [1 ]
Imbach, P [1 ]
机构
[1] Novartis, Oncol Res Dept, CH-4002 Basel, Switzerland
关键词
cyclin-dependent kinase; CDK1; inhibitor; olomoucine; structure-based design;
D O I
10.1023/A:1008115004986
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Cyclin-dependent kinase 1 (CDK1), an enzyme participating in the regulation of the cell cycle, constitutes a possible target in the search for new antitumor agents. Starting from the purine derivative olomoucine and following a structure-based approach, potent inhibitors of this enzyme were rapidly identified. The molecular modeling aspects of this work are described.
引用
收藏
页码:403 / 409
页数:7
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