AbstractObjective:As a result of adverse effects including drug-resistance, toxicity and low bioavailability, there has been a crucial need for novel anticancer agents. In this present study, some novel 2,5-disubstituted 1,3,4-oxadiazole derivatives bearing pyridine moiety were synthesized and their potential cytotoxic activities were examined.Materials and methods:A series of seven new compounds of 2-[(5-(3-(pyrimidin-2-yl)thio)propyl)-1,3,4-oxadiazol-2-yl)thio)]-1-(4-substituted)ethan-1-one derivatives were synthesized by reacting 5-[(3-(pyrimidin-2-yl)thio)propyl]-1,3,4-oxadiazole-2-thiol and 4-substituted phenacyl bromide derivatives in acetone with potassium carbonate. The structures of the obtained compounds were elucidated using FT-IR,Results:Among the tested compounds, compoundConclusions:It was determined that some of synthesized compounds had considerable anticancer activity against the A549 cell lines. Compound