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

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

Volume: 11 Issue: 8

Author(s): 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:

Keywords: 1-(Benzofuran-2-yl)methyl, Cytotoxic activity, Hybrid compound, Structure-activity relationships, Triazole.

Abstract: 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.

Cite this article as:

Shi Yi-Min, Yang Li-Juan, Chen Wen, Sun Cheng-Jun, Xu Xiao-Liang, Zhou Shu-Ya, Zhang Hong- Bin and Yang Xiao-Dong, Synthesis and Biological Activity of Novel 1-((benzofuran-2-yl)methyl)-1Htriazole Derivatives, Letters in Drug Design & Discovery 2014; 11 (8) . https://dx.doi.org/10.2174/1570180811666140423214501