Synthesis and antitumor activity of novel 2-substituted indoline imidazolium salt derivatives
Xiao-Liang Xu1, Chun-Lei Yu, Wen Chen
1Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming, 650091, P. R. China. xdyang@ynu.edu.cn zhanghbyd@gmail.com.
Abstract:
A series of novel 2-substituted indoline imidazolium salt derivatives has been prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the existence of a substituted benzimidazole ring and substitution of the imidazolyl-3-position with a naphthylacyl or 2-naphthylmethyl group were vital for modulating the cytotoxic activity. Compound 25 was found to be the most potent derivative with IC50 values of 0.24-1.18 μM, and exhibited cytotoxic activity selectively against MCF-7, SW480, SMMC-7721 and HL-60 cell lines, while compound 26 showed powerful inhibitory activities selectively against SMMC-7721 and A549 cell lines. Compound 25 can induce G2/M phase cell cycle arrest and apoptosis in SMMC-7721 cells.
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