期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 87, 期 -, 页码 306-315出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.09.071
关键词
Synthesis; Antiproliferative activity; Tubulin; Benzimidazole carbamates; Indole; Docking
资金
- National ST Major Project [2012ZX09103101-060]
- National Natural Science Foundation of China [30973614]
- Excellent Talent Supporting Project of Liaoning Province [LR20013046]
- Ministry of Education
- Program for Liaoning Innovative Research Team in University
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.
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