Design and Synthesis of Sulfonamide-1, 2, 3-Triazole Derivatives Bearing a Dithiocarbamate Moiety as Antiproliferative Agents. (September 2017)

• Record Type: Journal Article
• Authors: Fu, Dong-Jun; Liu, Ying-Chao; Yang, Jia-Jia; Zhang, Ji; Xiong, Chao-Dong; Cao, Zhu-Song; Yin, Xu-Xu; Wei, Wei; Zhang, Yan-Bing
• Is Part Of: Journal of chemical research. Volume 41:Number 9(2017)
• Page Start: 523
• Page End: 525
• Publication Date: 2017-09
• Subjects: antiproliferative activity -- sulfonamide-1, 2, 3-triazole -- dithiocarbamate; Chemistry -- Research -- Periodicals; Chemistry -- Periodicals; 540.5
• DOI: 10.3184/174751917X15027935057950
• Languages: English
• ISSNs: 1747-5198

Abstract

A series of nine novel 1-(4′-sulfamoylphenyl)-1, 2, 3-triazole derivatives bearing a 4-dithiocarbamylmethyl moiety were designed using the molecular hybridisation approach and synthesised by alkyne/azide click chemistry. Most of the synthesised compounds exhibited moderate to good antiproliferative activity against oesophagus, gastric and prostate cancer cell lines, but a compound containing a 4-( t -butoxycarbonyl)piperazinylthiocarbonyl moiety showed the highest activity. Against a prostate cancer cell line, it had an IC50 value of 2.4 μM, about 10-fold more active than 5-flurouracil. This work shows that novel sulfonamide-1, 2, 3-triazole derivatives bearing a dithiocarbamate moiety linked to a 4-substituted piperazine are promising lead compounds for the development of antitumour agents.