Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 19, Issue 8, Pages 2659-2665Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.03.005
Keywords
Chalcones; Cytotoxicity; Tubulin polymerization; Molecular modeling
Funding
- Knut and Alice Wallenberg Foundation
- Swedish Research Council [621-2010-4846]
- Academy of Finland
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A series of dihalogenated chalcones and structurally related dienones were synthesized and evaluated for their antiproliferative activity in 10 different cancer cell lines and for their effect on microtubule assembly. All compounds showed cytotoxic activity, with IC50 values in the 5-280 mu M range depending on the chalcone structure and the cell line. Five of the compounds were found to be tubulin polymerization inhibitors. In contrast, one of the compounds was found to stabilize tubulin to the same extent as the anticancer drug docetaxel. Molecular modeling suggested that the tubulin inhibitors bind to the colchicine binding site of beta-tubulin while the novel tubulin stabilization agent seems to interact with the paclitaxel binding site. (C) 2011 Elsevier Ltd. All rights reserved.
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