Synthesis and Biological Evaluation of Novel 5,7-Diphenylimidazo[1,2-a]pyridine Derivatives

doi:10.1007/s40242-014-4081-3

高等学校化学研究 ›› 2014, Vol. 30 ›› Issue (5): 759-763.doi: 10.1007/s40242-014-4081-3

Synthesis and Biological Evaluation of Novel 5,7-Diphenylimidazo[1,2-a]pyridine Derivatives

LIAO Huimin, CHONG Lian'e, TAN Li, CHEN Xiaodan, YOU Rui, GONG Ping

Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China

收稿日期:2014-03-10 修回日期:2014-03-24 出版日期:2014-10-01 发布日期:2014-05-12
通讯作者: GONG Ping E-mail:gongpinggp@126.com
基金资助:
Supported by the National Natural Science Foundation of China(No.81273357).

Synthesis and Biological Evaluation of Novel 5,7-Diphenylimidazo[1,2-a]pyridine Derivatives

LIAO Huimin, CHONG Lian'e, TAN Li, CHEN Xiaodan, YOU Rui, GONG Ping

Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China

Received:2014-03-10 Revised:2014-03-24 Online:2014-10-01 Published:2014-05-12
Contact: GONG Ping E-mail:gongpinggp@126.com
Supported by:
Supported by the National Natural Science Foundation of China(No.81273357).

摘要/Abstract

摘要：

A series of novel 5,7-diphenylimidazo[1,2-a]pyridine derivatives was designed and synthesized. The in vitro cytotoxic activities of all the target compounds against human colorectal cancer(HT-29), human lung cancer(H460), human gastric cancer(MKN45) and human breast cancer(MDA-MB-231) cell lines were evaluated. The pharmacological results indicated thatmost of the target compounds showed moderate to excellent activities against the tested cell lines. The most promising compound 4h(0.20, 0.006, 0.08, 0.021 μmol/L) was 2.6, 5.1, 3.6 and 21.9 times more active than EPC2407(0.52, 0.031, 0.29, 0.46 μmol/L) against HT-29, H460, MKN45 and MDA-MB-231 cell lines, respectively.

关键词: Imidazo[1,2-a]pyridine, Biological evaluation, Antitumor activity

Abstract:

Key words: Imidazo[1,2-a]pyridine, Biological evaluation, Antitumor activity

LIAO Huimin, CHONG Lian'e, TAN Li, CHEN Xiaodan, YOU Rui, GONG Ping. Synthesis and Biological Evaluation of Novel 5,7-Diphenylimidazo[1,2-a]pyridine Derivatives[J]. 高等学校化学研究, 2014, 30(5): 759-763.

LIAO Huimin, CHONG Lian'e, TAN Li, CHEN Xiaodan, YOU Rui, GONG Ping. Synthesis and Biological Evaluation of Novel 5,7-Diphenylimidazo[1,2-a]pyridine Derivatives[J]. Chemical Research in Chinese Universities, 2014, 30(5): 759-763.

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Synthesis and Biological Evaluation of Novel 5,7-Diphenylimidazo[1,2-a]pyridine Derivatives

Synthesis and Biological Evaluation of Novel 5,7-Diphenylimidazo[1,2-a]pyridine Derivatives

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