2. Academic Validation
  3. Discovery of novel 2-phenyl-imidazo[1,2-a]pyridine analogues targeting tubulin polymerization as antiproliferative agents

Discovery of novel 2-phenyl-imidazo[1,2-a]pyridine analogues targeting tubulin polymerization as antiproliferative agents

  • Eur J Med Chem. 2016 Apr 13;112:367-372. doi: 10.1016/j.ejmech.2016.02.004.
Weiteng An 1,  Wei Wang 1,  Ting Yu 1,  Yongliang Zhang 1,  Zehong Miao 2,  Tao Meng 3,  Jingkang Shen 4
Affiliations

Affiliations

  • 1 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China.
  • 2 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China. Electronic address: zhmiao@simm.ac.cn.
  • 3 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China. Electronic address: tmeng@sibs.ac.cn.
  • 4 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China. Electronic address: jkshen@simm.ac.cn.
PMID: 26927488 DOI: 10.1016/j.ejmech.2016.02.004
Abstract

A series of 2-aryl-imidazo-pyridines/pyrazines derivatives has been designed, synthesized and evaluated for their biological activities. Among them, several investigated compounds (1a, 3b and 3d) displayed potent antiproliferative activity against HeLa cell, and also displayed comparable tubulin polymerization inhibitory activity to colchicine. These studies provided a new molecular scaffold for the further development of antitumor agents that target tubulin.

Keywords

Anticancer agents; Colchicine binding site; Intra-molecular hydrogen bonding; Tubulin inhibitor.

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