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Combretastatin-like chalcones as inhibitors of microtubule polymerization. Part 1: synthesis and biological evaluation of antivascular activity.

Ducki, S, Renninson, D, Woo, M, Kendall, A, Mcgown, A and Lawrence, NJ 2009, 'Combretastatin-like chalcones as inhibitors of microtubule polymerization. Part 1: synthesis and biological evaluation of antivascular activity.' , Bioorganic and Medicinal Chemistry, 17 (22) , pp. 7698-7710.

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Abstract

The alpha-methyl chalcone SD400 is a potent inhibitor of tubulin assembly and possesses potent anticancer activity. Various chalcone analogues were synthesized and evaluated for their cell growth inhibitory properties against the K562 human chronic myelogenous leukemia cell line (SD400, IC(50) 0.21nM; combretastatin A4 CA4, IC(50) 2.0nM). Cell cycle analysis by flow cytometry indicated that these agents are antimitotic (SD400, 83% of the cells are in G(2)/M phase; CA4 90%). They inhibit tubulin assembly at low concentration (SD400, IC(50) 0.46microM; CA4, 0.10microM) and compete with [(3)H]colchicine for binding to tubulin (8% [(3)H]colchicine remained bound to tubulin after competition with SD400 or CA4). Upon treatment with SD400, remarkable cell shape changes were elicited in HUVEC cells, consistent with vasculature damaging activity

Item Type: Article
Uncontrolled Keywords: Chalcone; Combretastatin; Tubulin; Antivascular; Anticancer; Colchicine; SD400
Themes: Subjects / Themes > Q Science > QD Chemistry
Subjects / Themes > R Medicine > RM Therapeutics. Pharmacology
Health and Wellbeing
Subjects outside of the University Themes
Schools: Colleges and Schools > College of Science & Technology
Colleges and Schools > College of Science & Technology > School of Environment and Life Sciences
Colleges and Schools > College of Science & Technology > School of Environment and Life Sciences > Biomedical Research Centre
Journal or Publication Title: Bioorganic and Medicinal Chemistry
Publisher: Elsevier
Refereed: Yes
ISSN: 0968-0896
Depositing User: AT McGown
Date Deposited: 16 Mar 2010 14:00
Last Modified: 20 Aug 2013 17:04
URI: http://usir.salford.ac.uk/id/eprint/3303

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