A Novel Method to Synthesize 4-Aryl-1H-1,2,3-Triazoles and its Antihepatoma Activity

Author(s): Xiaolong Li, Yun He, Li Hai, Tao Zhang, Yong Wu.

Journal Name: Anti-Cancer Agents in Medicinal Chemistry

Volume 16 , Issue 12 , 2016

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Abstract:

A novel synthetic method of 4-substituted aryl-1H-1,2,3-triazoles from arylglyoxaldoxime semicarbazone with sodium dithionite and O2 was found to be safer than the Huisgen azide– alkyne dipolar cycloaddition. A total of 17 new structures of 4-substituted aryl-1H-1,2,3- triazoles were characterized by 1H NMR, 13C NMR, ESI-MS. Subsequently, their in vitro antihepatoma activities were evaluated on human hepatoma QGY-7703, Bel-7402 and SMMC-7721 cell lines and mouse fibroblast cells L-929 by MTS assay. Among them, 5k exhibited excellent activity against QGY-7703 (GI50 = 0.0232 μM), while 5p and 5q displayed good activity (GI50 = 0.103 μM and GI50 = 0.182 μM) against the growth of SMMC-7721 cell lines. Furthermore, 5k, 5p and 5q showed slight selectivity of inhibition on hepatoma cell lines over normal cell line L-929.

Keywords: Synthesis, anti-hepatoma activity, sodium dithionite, O2, 4-aryl-1H-1, 2, 3-triazoles, anti-hepatoma activity.

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Article Details

VOLUME: 16
ISSUE: 12
Year: 2016
Page: [1622 - 1627]
Pages: 6
DOI: 10.2174/1871520616666151123095646
Price: $58

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