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.