Chemical Research in Chinese Universities ›› 2014, Vol. 30 ›› Issue (5): 759-763.doi: 10.1007/s40242-014-4081-3

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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   

  1. 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).

Abstract:

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.

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