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

…, D Rennison, M Woo, A Kendall, JFD Chabert…

Index: Ducki, Sylvie; Rennison, David; Woo, Meiko; Kendall, Alexander; Chabert, Jeremie Fournier Dit; McGown, Alan T.; Lawrence, Nicholas J. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 22 p. 7698 - 7710

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Citation Number: 106

Abstract

The α-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, IC50 0.21 nM; combretastatin A4 CA4, IC50 2.0 nM). Cell cycle analysis by flow cytometry indicated that these agents are antimitotic (SD400, 83% of the ...