Design and Synthesis of Sulfonamide-1,2,3-Triazole Derivatives Bearing a Dithiocarbamate Moiety as Antiproliferative Agents

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.

Discovery of novel mRNA demethylase FTO inhibitors against esophageal cancer

“…1,2,3-Triazole-pyridine hybrids C1 ∼ C8 were evaluated for their antiproliferative activities against five esophageal cancer cell lines (KYSE-150, KYSE-270, TE-1, KYSE-510, and EC109) by the MTT assay. 5-Fluorouracil (5-Fu) was employed as the reference drug in the reported reference for the antiproliferative evaluation of 1,2,3-triazole derivatives 15 . So, it also was used as the control to evaluate the accuracy of antiproliferative results.…”