Design and synthesis of 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles and pyrazolo[3,4-b]pyridines for Aurora-A kinase inhibitors

被引：25
|
作者：
Shi, Jianyou [1 ,2 ,3 ]
Xu, Guobin [1 ,2 ]
Zhu, Wei [1 ,2 ]
Ye, Haoyu [1 ,2 ]
Yang, Shengyong [1 ,2 ]
Luo, Youfu [1 ,2 ]
Han, Jing [1 ,2 ]
Yang, Jincheng [1 ,2 ,3 ]
Li, Rui [1 ,2 ,4 ]
Wei, Yuquan [1 ,2 ]
Chen, Lijuan [1 ,2 ]
机构：
[1] Sichuan Univ, W China Med Sch, W China Hosp, State Key Lab Biotherapy, Chengdu 610041, Sichuan, Peoples R China
[2] Sichuan Univ, W China Med Sch, W China Hosp, Ctr Canc, Chengdu 610041, Sichuan, Peoples R China
[3] Sichuan Univ, Pharm Coll W China, Chengdu 610065, Sichuan, Peoples R China
[4] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 14期
基金：
美国国家科学基金会;
关键词：
1,4,5,6-Tetrahydropyrrolo[3,4-c]pyrazoles; Pyrazolo[3,4-b]pyridines; Antitumor; Aurora-A kinase; POTENT; DISCOVERY; PROFILE;
D O I：
10.1016/j.bmcl.2010.04.083
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Two series of 3-aminopyrazole compounds including 24 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles and 16 pyrazolo[3,4-b]pyridines were synthesized and evaluated against HCT116, A549, and A2780 tumor cell lines. Among them, three compounds were found to have the ideal anti-proliferative activities in vitro. Docking experiments showed that the novel pyrazolo[3,4-b]pyridines share the similar interaction mode with Aurora-A kinase as PHA739358. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4273 / 4278
页数：6
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