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

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

Volume: 16 Issue: 12

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

Affiliation:

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

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.

Cite this article as:

Li Xiaolong, He Yun, Hai Li, Zhang Tao and Wu Yong, A Novel Method to Synthesize 4-Aryl-1H-1,2,3-Triazoles and its Antihepatoma Activity, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (12) . https://dx.doi.org/10.2174/1871520616666151123095646