Design, synthesis, and structure–activity relationship studies of novel millepachine derivatives as potent antiproliferative agents

…, Y Sang, X Liang, Y Ran, A Peng, Y Wei, L Chen

文献索引：Wang, Guangcheng; Wu, Wenshuang; Peng, Fei; Cao, Dong; Yang, Zhuang; Ma, Liang; Qiu, Neng; Ye, Haoyu; Han, Xiaolei; Chen, Jinying; Qiu, Jingxiang; Sang, Yun; Liang, Xiaolin; Ran, Yan; Peng, Aihua; Wei, Yuquan; Chen, Lijuan European Journal of Medicinal Chemistry, 2012 , vol. 54, p. 793 - 803

全文：HTML全文

被引用次数: 16

摘要

In this paper, 38 millepachine derivatives have been designed, synthesized and evaluated for their in vitro and in vivo antiproliferative activity. Among these novel derivatives, 15 displayed more potent antiproliferative activity than millepachine against HepG2, K562, SK- OV-3, HCT116, HT29, and SW620 tumor cells (mean IC50= 0.64 vs. 2.86 μM, respectively). Furthermore, 15 could effectively inhibit tubulin polymerization in HepG2 cells, and induce ...