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

Index: 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

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Citation Number: 16

Abstract

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 ...