Letters in Drug Design & Discovery

Atta-ur-Rahman  , FRS
Honorary Life Fellow
Kings College
University of Cambridge
Email: lddd@benthamscience.org


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

Author(s): Yi-Min Shi, Li-Juan Yang, Wen Chen, Cheng-Jun Sun, Xiao-Liang Xu, Shu-Ya Zhou, Hong- Bin Zhang, Xiao-Dong Yang.

Graphical 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.

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

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Article Details

Year: 2014
Page: [975 - 984]
Pages: 10
DOI: 10.2174/1570180811666140423214501
Price: $58