Synthesis and Biological Activity of Novel 1-((Benzofuran-2-yl)Methyl)–1H-Triazole Derivatives

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

Volume 11, 10 Issues, 2014

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Letters in Drug Design & Discovery

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Atta-ur-Rahman, FRS
Honorary Life Fellow
Kings College
University of Cambridge

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Synthesis and Biological Activity of Novel 1-((Benzofuran-2-yl)Methyl)–1H-Triazole Derivatives

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 Medicinal Chemistry for Natural Resource Ministry of Education Yunnan University 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: Hybrid compound, 1-(Benzofuran-2-yl)methyl, Triazole, Cytotoxic activity, Structure-activity relationships

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Article Details

Volume: 11
First Page: 1
Last Page: 10
Page Count: 10
DOI: 10.2174/1570180811666140423214501

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