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

ISSN: 1875-628X (Online)
ISSN: 1570-1808 (Print)

Volume 14, 12 Issues, 2017

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Letters in Drug Design & Discovery

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G. Perry
University of Texas
San Antonio, TX

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

Letters in Drug Design & Discovery, 11(8): 975-984.

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: 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.


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

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Article Details

Volume: 11
Issue Number: 8
First Page: 975
Last Page: 984
Page Count: 10
DOI: 10.2174/1570180811666140423214501
Price: $58

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