Design, synthesis and biological evaluation of chrysin benzimidazole derivatives as potential anticancer agents

作者：Wang, Zhe; Deng, Xiangping; Xiong, Shujuan; Xiong, Runde; Liu, Juan; Zou, Liu; Lei, Xiaoyong; Cao, Xuan; Xie, Zhizhong; Chen, Yanming; Liu, Yunmei; Zheng, Xing^*; Tang, Guotao^*

来源：Natural Product Research, 2018, 32(24): 2900-2909.

DOI：10.1080/14786419.2017.1389940

• Chrysin
• benzimidazole
• synthesis
• anticancer

A series of chrysin benzimidazole derivatives were synthesised and evaluated for their anticancer activity in the search for potential anticancer agents. Among them, compound 18 displayed the most potent anti-proliferative activity against MFC cells with IC50 values of 25.72 +/- 3.95 mu M. The flow cytometry results displayed that compound 18 induced apoptosis of MFC cells in a dose-dependent manner and caused the cell cycle to be arrested in the G0/G1 phase. Furthermore, the preliminary anticancer activity in vivo was also studied in tumour-bearing mice, and the compound 18 exerted good inhibition effect on tumour growth. These results suggested that compound 18 had good anticancer activity, which could be a potential anticancer agent after further optimisation and evaluation. @@@ [GRAPHICS] @@@ .

• 出版日期2018-12-17
• 单位南华大学