Design, synthesis and biological evaluation of a novel series of 1,3,4-oxadiazole bearing N-methyl-4-(trifluoromethyl)phenyl pyrazole moiety as cytotoxic agents

On account of the reported anticancer activity of pyrazoles and oxadiazoles, we have designed and synthesized a novel combinatorial library of S-substituted-1,3,4-oxadiazole bearing N-methyl-4-(trifluoromethyl)phenyl pyrazole moiety and tested for in-vitro cytotoxic activity by MTT assay. Amongst the tested compounds, the compound 5e was the most promising anticancer agent with IC50 value of 15.54 μM in MCF-7 cells, compared to Doxorubicin as standard drug. The newly synthesized compounds were characterized by NOE, IR, 1H NMR, 13C NMR and LC–MS analysis.

Graphical abstractA novel combinatorial library of S-substituted-1,3,4-oxadizole bearing N-methyl-4-(trifluoromethyl)phenyl pyrazole moiety were designed, synthesized and screened for their cytotoxic activity using MTT assay.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► A novel series of 1,3,4-oxadiazoles bearing N-methylpyrazoles were synthesized. ► Compounds were tested for their cytotoxic activity by MTT assay. ► Compound 5e is the most promising cytotoxic agent.