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Inhibitors and promoters of tubulin polymerization: Synthesis and biological evaluation of chalcones and related dienones as potential anticancer agents
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Medical Sciences, Clinical Pharmacology.
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2011 (English)In: Bioorganic & Medicinal Chemistry, ISSN 0968-0896, E-ISSN 1464-3391, Vol. 19, no 8, 2659-2665 p.Article in journal (Refereed) Published
Abstract [en]

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.

Place, publisher, year, edition, pages
2011. Vol. 19, no 8, 2659-2665 p.
Keyword [en]
Chalcones, Cytotoxicity, Tubulin polymerization, Molecular modeling
National Category
Medical and Health Sciences
Identifiers
URN: urn:nbn:se:uu:diva-152919DOI: 10.1016/j.bmc.2011.03.005ISI: 000289281600019PubMedID: 21459004OAI: oai:DiVA.org:uu-152919DiVA: diva2:414422
Available from: 2011-05-03 Created: 2011-05-03 Last updated: 2017-12-11Bibliographically approved

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