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

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 IC50 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 the minor groove of DNA.

Graphical abstractA new series of bis-benzimidazole derivatives were synthesized, and these compounds exhibited high anti-tumor activity by binding into the minor groove of DNA.Figure optionsDownload full-size imageDownload as PowerPoint slide