Synthesis and evaluation of 2,5-di(4-aryloylaryloxymethyl)-1,3,4-oxadiazoles as anti-cancer agents

A series of 2,5-di(4-aryloylaryloxymethyl)-1,3,4-oxadiazoles 9a–j were obtained via multistep synthesis from hydroxybenzophenones 4a–e. The cytotoxicity of compounds 9a–j was evaluated against human leukemia cell lines (K562 and CEM). The compounds exhibited moderate to good anti-cancer activity with compounds 9b and 9i having a chloro group exhibiting the best activity (IC50 = 10 μM). Compound 9i exhibited activity against both the cell lines and 9b only exhibited activity against CEM. Further, a lactate dehydrogenase (LDH) assay and DNA fragmentation studies of the compounds 9a–j were also performed. [Display omitted] 2,5-Di(4-aryloylaryloxymethyl)-1,3,4-oxadiazoles 9a–j were synthesized and examined for cytotoxicity on human leukemia cell lines. Further, a lactate dehydrogenase assay and DNA fragmentation studies were also performed. ► Synthesis of biologically active analogs of 1,3,4-oxadiazoles was carried out. ► Cytotoxicity of the synthesized compounds was evaluated against human leukemia cell lines. ► Compounds exhibited moderate to good anti-cancer activity. ► Lactate dehydrogenase assay and DNA fragmentation studies were also performed.