Synthesis of new chiral 2,5-disubstituted 1,3,4-thiadiazoles possessing γ-butenolide moiety and preliminary evaluation of in vitro anticancer activity

A new series of chiral 1,3,4-thiadiazoles derivatives possessing γ-substituted butenolide moiety were synthesized and evaluated for in vitro anticancer properties. All the compounds showed good anticancer activities against Hela cell lines. Of all the studied compounds, compound 9e exhibited the best inhibitory activity with an IC50 of 0.9 μM. After being treated with 0.1 μg/mL compound 9e for 24 h, the growth inhibition rate of Hela cell lines was 59.2%.

Graphical abstractIn the present study, a new series of chiral 2,5-disubstituted 1,3,4-thiadiazoles possessing γ-butenolide moiety were synthesized and evaluated for their in vitro anticancer activity.Figure optionsDownload full-size imageDownload as PowerPoint slide