Design and synthesis of novel 1,2,3-triazole-dithiocarbamate hybrids as potential anticancer agents

A series of novel 1,2,3-triazole-dithiocarbamate hybrids were designed, synthesized and evaluated for anticancer activity against four selected human tumor cell lines (MGC-803, MCF-7, PC-3, EC-109). Majority of the synthesized compounds exhibited moderate to potent activity against MGC-803 and MCF-7. Among them, compounds 3a and 3c showed excellent broad spectrum anticancer activity with IC50 values ranging from 0.73 to 11.61 μM and 0.49–12.45 μM, respectively. Particularly, compound 3a was more potent than 5-fluorouracil against all tested human cancer cell lines. Flow cytometry analysis demonstrated that treatment of MGC-803 with 3c led to cell cycle arrest at G2/M phase accompanied by an increase in apoptotic cell death after 12 h.

The novel 1,2,3-triazole-dithiocarbamate hybrids 3a and 3c exhibited excellent broad spectrum anticancer activity with IC50 values ranging from 0.73 to 11.61 μM and 0.49–12.45 μM, respectively.Figure optionsDownload as PowerPoint slideHighlights
► A series of novel 1,2,3-triazole-dithiocarbamate hybrids were synthesized.
► Majority of the compounds showed potent anticancer activity against MGC-803 and MCF-7.
► Compounds 3a and 3c exhibited remarkable broad spectrum anticancer activity.
► Compound 3c showed cell cycle arrest at G2/M phase and induced apoptosis.
► These hybrids have simple structures and are easy to synthesize.