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

TitleDesign, synthesis and antiproliferative activity studies of novel 1,2,3-triazole-dithiocarbamate-urea hybrids.
Publication TypeJournal Article
Year of Publication2013
AuthorsDuan Y-C, Zheng Y-C, Li X-C, Wang M-M, Ye X-W, Guan Y-Y, Liu G-Z, Zheng J-X, Liu H-M
JournalEuropean journal of medicinal chemistry
Volume64
Pagination99-110
Date Published2013 Jun
Abstract

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.

DOI10.1038/nm.3162
Alternate JournalEur J Med Chem