Discovery of novel 2-phenyl-imidazo[1,2-a]pyridine analogues targeting tubulin polymerization as antiproliferative agents
作者:Weiteng An、Wei Wang、Ting Yu、Yongliang Zhang、Zehong Miao、Tao Meng、Jingkang Shen
DOI:10.1016/j.ejmech.2016.02.004
日期:2016.4
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.
已经设计,合成并评估了一系列2-芳基-咪唑并吡啶/吡嗪衍生物的生物学活性。其中,几种研究的化合物(1a,3b和3d)显示出对HeLa细胞的有效抗增殖活性,并且还显示出与秋水仙碱相当的微管蛋白聚合抑制活性。这些研究为靶向微管蛋白的抗肿瘤药物的进一步开发提供了新的分子支架。