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Paper | Regular issue | Vol 85, No. 9, 2012, pp.2231-2240
Published online, 20th July, 2012
DOI: 10.3987/COM-12-12521
A New Series of Bisbenzimidazole Derivatives: Synthesis, Antitumor Activity and Low Toxicity on PBMC

Xiu-Jun Wang, Qing-He Wang,* Chao Liu, Wei Li, Jian Wang, Na Yang, and Mao-Sheng Cheng*

*School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China

Abstract

Herein, a new series of bisbenzimidazole 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 µM for U937 tumor cell line, 5.62 µM for HL60 tumor cell line and 6.97 µM 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.