Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 23, Pages 8218-8225Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.10.008
Keywords
Chalcone; Guanidine; Molecular modeling; Antitubulin polymerization
Funding
- Jiangsu National Science Foundation [BK2009239]
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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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