Bioorganic & Medicinal Chemistry 2008-03-01

Synthesis and biological evaluation of imidazol-2-one derivatives as potential antitumor agents.

Na Xue, Xiaochun Yang, Rui Wu, Jing Chen, Qiaojun He, Bo Yang, Xiuyang Lu, Yongzhou Hu

文献索引：Bioorg. Med. Chem. 16(5) , 2550-7, (2008)

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摘要

A new series of aryl substituted imidazol-2-one derivatives structurally related to combretastatin A-4 (CA-4) were synthesized and evaluated for their cytotoxic activities in vitro against various human cancer cell lines including MDR cell line. The cytotoxic effects of compounds 7b and 7i proved to be similar to or greater than that of docetaxel. The highly active compound 7b also exhibited excellent inhibitory activity on tumor growth in vivo.