Synthesis and evaluation of benzimidazole carbamates bearing indole moieties for antiproliferative and antitubulin activities
Synthesis and evaluation of benzimidazole carbamates bearing indole moieties for antiproliferative and antitubulin activities
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DOI：
10.1016/j.ejmech.2014.09.071
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发表时间：
2014-11-24
影响因子：
6.7
通讯作者：
Zhang, Weige
中科院分区：
文献类型：
--
作者：
Guan, Qi;Han, Chunming;Zhang, Weige
合成了一系列含硫或硒原子连接芳香环的吲哚基团的新型苯并咪唑氨基甲酸酯，并评价了它们对三种人类癌细胞（SGC-7901）的抗增殖活性。A-549和HT-1080)使用MTT试验。化合物10a、10b、7a、7b和7f对这些细胞系有明显的抑制作用。我们选择了该系列中最有效的化合物10a来研究其抗肿瘤机制。此外，分子对接研究表明，化合物10a通过在微管蛋白的秋水仙碱结合位点的氢键与nocodazole对接位有非常密切的相互作用。(C) 2014 Elsevier Masson SAS。版权所有。
A series of novel benzimidazole carbamates bearing indole moieties with sulphur or selenium atoms connecting the aromatic rings were synthesised and evaluated for their antiproliferative activities against three human cancer cell lines (SGC-7901. A-549 and HT-1080) using an MTT assay. Compounds 10a, 10b, 7a, 7b and 7f showed significant activities against these cell lines. The most potent compound in this series, 10a, was selected to investigate its antitumour mechanism. In addition, molecular docking studies suggested that compound 10a interacts very closely with the nocodazole docking pose through hydrogen bonds at the colchicine binding site of tubulin. (C) 2014 Elsevier Masson SAS. All rights reserved.