Abstract
A series of novel hybrid compounds between 2-alkylbenzofuran and imidazole has been prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the existence of 2-methyl-imidazole or 2-ethyl-imidazole ring and substitution of the imidazolyl-3-position with a naphthylacyl or methoxyphenacyl group were vital for modulating cytotoxic activity. In particular, hybrid compound 29 was found to be the most potent compound against five strains human tumor cell lines and more active than cisplatin (DDP), while hybrid compound 26 was more selective toward colon carcinoma (SW480) and breast carcinoma (MCF-7) with IC50 value 44.0- and 36.8-fold more sensitive to DDP.
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