Design of novel bis-benzimidazole derivatives as DNA minor groove binding agents

XJ Wang, ML Yang, LP Zhang, T Yao, C Chen…

Index: Wang, Xiu-Jun; Yang, Ming-Li; Zhang, Lan-Ping; Yao, Tong; Chen, Cheng; Mao, Lian-Gang; Wang, Yin; Wu, Jie Chinese Chemical Letters, 2014 , vol. 25, # 4 p. 589 - 592

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Abstract

Abstract A new series of bis-benzimidazole derivatives were designed and synthesized. In vitro cytotoxicity evaluation showed that these compounds exhibited high activity against the selected tumor cells. Among them, compound 9 owned the best potential, its IC 50 values being 5.95 μmol/L (mononuclear tumor cell line (U937)) and 5.58 μmol/L (cervical cancer cell (HeLa)). Fluorescence and UV–vis studies showed that compound 9 could bind into ...