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

来源 :Chinese Chemical Letters | 被引量 : 0次 | 上传用户:wllzjw
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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 the minor groove of DNA. A new series of bis-benzimidazole derivatives were designed and synthesized. In vitro cytotoxicity evaluation showed those compounds exploring 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 the minor groove of DNA.
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