Synthesis and biological evaluation of disulfides bearing 1,2,4-triazole moiety as antiproliferative agents

Article abstract of DOI:10.1007/s00044-017-2029-0

A series of novel nonsymmetrical disulfides bearing 1,2,4-triazole moiety were designed, synthesized, and evaluated for their in vitro antiproliferative activities against human cancer cell lines SMMC-7721, Hela, A549, and normal cell lines L929 by CCK-8 assay. The preliminary bioassay results demonstrated that most of the tested compounds 8a–r exhibited good antiproliferative activities, and some compounds showed better effects than positive control 5-fluorouracil against various cancer cell lines. Among these compounds, compound 8l showed significant antiproliferative activity against SMMC-7721 cells with IC₅₀ value of 2.97 μM. Compound 8f displayed highly effective biological activity against Hela cells with IC₅₀ value of 3.51 μM. Compound 8d exhibited the best inhibitory effect against A549 cells with IC₅₀ value of 2.79 μM. Furthermore, some of the tested compounds showed weak cytotoxic effect against the normal cell lines L929. The pharmacological results suggest that the substituent groups are vital for improving the potency and selectivity of this class of compounds.