Title: Synthesis and antitumor activity of novel N-substituted tetrahydro-beta-carboline-imidazolium salt derivatives
First Author: Zhou, Bei; Liu, Zheng-Fen; Deng, Guo-Gang; Chen, Wen; Li, Min-Yan; Yang, Li-Juan; Li, Yan; Yang, Xiao-Dong; Zhang, Hong-Bin
Abstract: The synthesis of a series of novel N-substituted tetrahydro-beta-carboline-imidazolium salt derivatives is presented. The biological properties of the compounds were evaluated in vitro against a panel of human tumor cell lines. The results suggest that the benzimidazole ring and 1-(naphthalen-2-yl) ethan-1-one or 2-naphthylmethyl substituent at the imidazolyl-3-position were vital for modulating cytotoxic activity. Compound 41 was observed as a potent derivative with IC50 values of 3.24-8.78 mu M and exhibited cytotoxic activity selectively against HL-60, A-549 and MCF-7 cell lines. Meanwhile, high inhibitory activities selectively against HL-60 and MCF-7 cell lines were observed for compound 51. Moreover, compound 51 was able to induce G1 phase cell cycle arrest and apoptosis in MCF-7 cells. The cytotoxicity of compound 51 against human normal lung epithelial cell line BEAS-2B was further evaluated.
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Page Number: 9423-9430
Issue: 39
Subject: Chemistry
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PubYear: 2016
Volume: 14
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