Xue Na, Yang Xiaochun, Wu Rui, Chen Jing, He Qiaojun, Yang Bo, Lu Xiuyang, Hu Yongzhou
ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
Bioorg Med Chem. 2008 Mar 1;16(5):2550-7. doi: 10.1016/j.bmc.2007.11.048. Epub 2007 Nov 22.
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.
合成了一系列与康普瑞他汀A-4（CA-4）结构相关的芳基取代咪唑-2-酮衍生物，并评估了它们在体外对包括多药耐药细胞系在内的各种人类癌细胞系的细胞毒活性。化合物7b和7i的细胞毒作用证明与多西他赛相似或更强。高活性化合物7b在体内对肿瘤生长也表现出优异的抑制活性。
