期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 18, 期 23, 页码 8218-8225出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.10.008
关键词
Chalcone; Guanidine; Molecular modeling; Antitubulin polymerization
资金
- Jiangsu National Science Foundation [BK2009239]
A series of novel chalcone guanidine derivatives (4a-4q) have been designed and synthesized, and their biological activity were also evaluated as potential antiproliferative and antitubulin polymerization inhibitors. Compound 4q showed the most potent biological activity (IC50 = 0.09 +/- 0.01 mu M for MCF-7 and IC50 = 8.4 +/- 0.6 mu M for tubulin), which is comparable to the positive controls. Docking simulation was performed to position compound 4q into the colchicine binding site to determine the probable binding model, which suggested probable inhibition mechanism. Published by Elsevier Ltd.
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