A NEW SERIES OF BISBENZIMIDAZOLE DERIVATIVES: SYNTHESIS, ANTITUMOR ACTIVITY AND LOW TOXICITY ON PBMC

[摘要]：Herein, a new series of bis-benzimidazole derivatives were designed and synthesized. Most of these new compounds showed significant in vitro anticancer activity when compared to Hoechst 33258 and 5-FU. Among them, the most potent compound 8 had the IC50 values of 0.78 mu M for U937 tumor cell line, 5.62 mu M for HL60 tumor cell line and 6.97 mu M for Hela tumor cell line. Molecular modeling, fluorescence and viscosimetry study showed that compound 8 could bind into the minor groove of DNA. Subsequent toxicity study on human peripheral blood mononuclear cells (PBMC), shows that compound 8 exhibited less toxicity than paclitaxel and 5-FU.

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