1204430-79-4Relevant academic research and scientific papers
Imidazolone-amide bridges and their effects on tubulin polymerization in cis-locked vinylogous combretastatin-A4 analogues: Synthesis and biological evaluation
Li, Yao-Wu,Liu, Jia,Liu, Na,Shi, Duo,Zhou, Xiao-Tian,Lv, Jia-Guo,Zhu, Ju,Zheng, Can-Hui,Zhou, You-Jun
, p. 3579 - 3584 (2011/07/09)
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′-NH2-4′-OCH 3, 4′-CH3 and 3′-CH3-substituted 1-phenyl B-ring, confer optimal bioactivity. The binding modes of these compounds to tubulin were obtained by molecular docking, which can explain the compounds' structure-activity relationship. The studies presented here provide a new structural type for the development of novel antitumor agents.
