Simplified staurosporine analogs as potent JAK3 inhibitors

被引：61
|
作者：
Yang, Shyh-Ming [1 ]
Malaviya, Ravi [1 ]
Wilson, Lawrence J. [1 ]
Argentieri, Rochelle [1 ]
Chen, Xin [1 ]
Yang, Cangming [1 ]
Wang, Bingbing [1 ]
Cavender, Druie [1 ]
Murray, William V. [1 ]
机构：
[1] Johnson & Johnson Pharmaceut Res & Dev LLC, Cranbury, NJ 08512 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 02期
关键词：
staurosporine; JAK3; Janus kinases 3;
D O I：
10.1016/j.bmcl.2006.10.062
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Simplification of bottom ring and regioselective functionalization of the indolocarbazole unit of staurosporine (2) are described. The modification led to a new series of simplified staurosporine analogs, which exhibited significant inhibitory activity against Janus kinase 3 (JAK3). The structure-activity relationships (SAR) are discussed and a proposed binding model is also highlighted. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：326 / 331
页数：6
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