Synthesis and CDK2 kinase inhibitory activity of 7/7′-azaindirubin derivatives

被引:0
作者
Zhao Hui Wang~a
机构
关键词
7’-Azaindirubin; 7-Azaindirubin; Synthesis; CDK2/cyclinA; Inhibition;
D O I
暂无
中图分类号
TQ464.8 [酶及辅酶];
学科分类号
100705 ;
摘要
A series of novel 7’-azaindirubin(1a-g) and 7-azaindirubin(2a,2c,2e and 2f) derivatives were designed and synthesized.Their structures were characterized by;H NMR and MS spectroscopy as well as by elemental analysis.Their inhibitory properties against CDK2/cylinA were evaluated in vitro.In contrast to indirubin,some of the described azaindirubins emerged as potent inhibitors of CDK2/cylinA and compound 2b had more potent activity.Biological tests also showed that nitrogen atom at 7-position of azaindirubin was more beneficial to enhance the kinase inhibitory activity.
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页码:297 / 300
页数:4
相关论文
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  • [2] Anti-mitotic properties of indirubin-3''-monoxime,a CDK/GSK-3 inhibitorinduction of endoreplication following prophase arrest .2 Damiens E,Baratte B,Marie D,et al. Oncogene . 2001