Synthesis and Biological Activity of Novel 1-((benzofuran-2-yl)methyl)-1Htriazole Derivatives
Yi-Min Shi, Li-Juan Yang, Wen Chen, Cheng-Jun Sun, Xiao-Liang Xu, Shu-Ya Zhou, Hong- Bin Zhang and Xiao-Dong Yang
Affiliation: Key Laboratory of Ethnic Medicine Resource Chemistry, Yunnan University of Nationalities, Kunming, Yunnan 650091, P. R. China.
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.
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