Synthesis and antitumor activity of novel 2-substituted indoline imidazolium salt derivatives

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-...

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Veröffentlicht in:Organic & biomolecular chemistry 2015-02, Vol.13 (5), p.1550-1557
Hauptverfasser: Xu, Xiao-Liang, Yu, Chun-Lei, Chen, Wen, Li, Ying-Chao, Yang, Li-Juan, Li, Yan, Zhang, Hong-Bin, Yang, Xiao-Dong
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Sprache:eng
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Zusammenfassung: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.
ISSN:1477-0520
1477-0539
DOI:10.1039/c4ob02385d