Design, synthesis and antiproliferative activity studies of novel 1,2,3-triazole–dithiocarbamate–urea hybrids

A series of novel 1,2,3-triazole–dithiocarbamate–urea hybrids were designed, synthesized and their antiproliferative activities against four selected human cancer cell lines were evaluated. The results showed that a number of the hybrids exhibited potent activity in selected human cancer cell lines. Among them, compounds 27 and 34 showed broad spectrum anticancer activity with IC50 values ranging from 1.62 to 20.84 μM and 0.76 to 13.55 μM, respectively. Interestingly, compounds 27 and 34, being very potent against MGC-803 cells, exhibited no significant cytotoxicity against normal human embryonic kidney cells at up to 55 μM and 70 μM, respectively. Evidences of cell cycle arrest and apoptosis induction were obtained for the most effective compounds 27 and 34 by means of flow cytometry and microscopic techniques. [Display omitted] Novel 1,2,3-triazole–dithiocarbamate–urea hybrids 34 exhibited potent anticancer activity with IC50 values ranging from 0.76 to 13.55 μM and was highly selective in its cytotoxicity activity. •A series of novel 1,2,3-triazole–dithiocarbamate–urea hybrids were synthesized.•Several compounds were more potent than 5-fluorouracil against MGC-803 and MCF-7.•Compounds 27 and 34 exhibited broad spectrum anticancer activity.•Compound 34 was highly selective in its cytotoxicity activity.•Compound 34 showed cell cycle arrest at G2/M phase and induced apoptosis.