Imidazolone–amide bridges and their effects on tubulin polymerization in cis-locked vinylogous combretastatin-A4 analogues: Synthesis and biological evaluation

…, N Liu, D Shi, XT Zhou, JG Lv, J Zhu, CH Zheng…

Index: Li, Yao-Wu; Liu, Jia; Liu, Na; Shi, Duo; Zhou, Xiao-Tian; Lv, Jia-Guo; Zhu, Ju; Zheng, Can-Hui; Zhou, You-Jun Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 11 p. 3579 - 3584

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Citation Number: 21

Abstract

Abstract A series of novel combretastatin-A4 analogues in which the cis-olefinic bridge is replaced by an imidazolone–amide were synthesized, and their cytotoxicity and tubulin- polymerization inhibitory activities were evaluated. These compounds appear to be potential tubulin-polymerization inhibitors. Compounds 10, 9b and 9c, bearing 3′-NH 2-4′-OCH 3, 4′-CH 3 and 3′-CH 3-substituted 1-phenyl B-ring, confer optimal bioactivity. The ...