Discovery of novel 2-phenyl-imidazo[1,2-a]pyridine analogues targeting tubulin polymerization as antiproliferative agents
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- 作者：Weiteng An1 ; Wei Wang1 ; Ting Yu ; Yongliang Zhang ; Zehong Miao ; zhmiao@simm.ac.cn" class="auth_mail" title="E-mail the corresponding author ; Tao Meng ; tmeng@sibs.ac.cn" class="auth_mail" title="E-mail the corresponding author ; Jingkang Shen ; jkshen@simm.ac.cn" class="auth_mail" title="E-mail the corresponding author
- 关键词：Anticancer agents ; Tubulin inhibitor ; Intra-molecular hydrogen bonding ; Colchicine binding site
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：13 April 2016
- 年：2016
- 卷：112
- 期：Complete
- 页码：367-372
- 全文大小：995 K
文摘
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Based on the iMHB approach, a novel series of 2-phenyl-imidazo[1,2-a]pyridine analogues were designed and synthesized.
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Compounds 1a, 3b, 3d were found to have excellent antiproliferative activities against HeLa cell.
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These compounds showed good tubulin polymerization inhibition activities.
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These studies provided a new class of antitubulin agents with the potential to be clinically developed for cancer treatment.