发现新型 2-苯基-咪唑并[1,2-a]吡啶类似物，作为针对微管聚合的抗增殖剂。
Discovery of novel 2-phenyl-imidazo[1,2-a]pyridine analogues targeting tubulin polymerization as antiproliferative agents.
机构信息
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China.
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China.
出版信息
Eur J Med Chem. 2016 Apr 13;112:367-372. doi: 10.1016/j.ejmech.2016.02.004. Epub 2016 Feb 5.
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.
设计、合成了一系列 2-芳基-咪唑并吡啶/吡嗪衍生物，并对它们的生物活性进行了评价。其中，几种研究化合物（1a、3b 和 3d）对 HeLa 细胞表现出很强的抗增殖活性，并且对微管蛋白聚合的抑制活性与秋水仙碱相当。这些研究为进一步开发以微管蛋白为靶点的抗肿瘤药物提供了新的分子骨架。
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