Design, synthesis and biological evaluation of novel hybrid compounds of imidazole scaffold-based 2-benzylbenzofuran as potent anticancer agents

• DOI: 10.1016/j.ejmech.2012.12.040
• Publication Date: 2013-01-03T18:47:52Z
• Authors: Xue-Quan Wang; Lan-Xiang Liu; Yan Li; Cheng-Jun Sun; Wen Chen; Liang Li; Hong-Bin Zhang; Xiao-Dong Yang
• Keywords: Imidazole; Benzimidazole

A series of novel hybrid compounds between 2-benzylbenzofuran and imidazole has been prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the existence of benzimidazole ring and substitution of the imidazolyl-3-position with a naphthylacyl or 4-methoxyphenacyl group were vital for modulating cytotoxic activity. In particular, hybrid compounds 46 and 47 were found to be the most potent derivatives against 5 strains human tumor cell lines and more active than cisplatin (DDP), and exhibited cytotoxic activities selectively against breast carcinoma (MCF-7) and myeloid liver carcinoma (SMMC-7721), respectively.