Synthesis and Biological Activity of Novel 1-((benzofuran-2-yl)methyl)-1Htriazole Derivatives

A series of novel 1-((benzofuran-2-yl)methyl)–1H-triazole derivatives has been synthesized and tested in vitro against a panel of five different human tumor cell lines. The results show that the existence of benzotriazole or 1,2,3- triazole ring and substitution of the triazolyl-3-position with a naphthylacyl, 4-bromophenacyl or 4-methylbenzyl group could be crucial for promoting cytotoxic activity. Compounds 18, 19, 20 and 25 were found to have the most potent activities selectively against HL-60, SMMC-7721 and MCF-7 cell lines respectively. In particular, compound 20 was more selective towards HL-60 and A549 cell lines with IC50 values of 0.62 and 1.60 µM. Keywords: 1-(Benzofuran-2-yl)methyl, Cytotoxic activity, Hybrid compound, Structure-activity relationships, Triazole.