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New α,β-unsaturated-2,5-disubstituted-1,3,4-Oxadiazoles  (4a–j)  and  (10a–d)  have been prepared in good to excellent yields starting from β-chlorovinyl aldehydes and hydrazide. The synthesized oxadiazoles were fully characterized by ( 1 H,  13 C) NMR, IR and HRM Sspectroscopic techniques. The  in vivo  antitumor activity of  4b ,  4c, 4g ,  4d , and  10c  was evaluated. Biochemical measurements of serum alanine aminotransferase, aspartate aminotransferase and creatinine levels of mice injected with a dose of 20 mg/kg, of each selected compound, showed no toxic effect, neither in liver nor in kidney organs. However, hepato/nephrotoxicities were observed in mice treated with a dose of 100 mg/kg. When tested on melanoma in a mice  xenograft  model, the pharmacodynamic study indicated that the two compounds  4c , bearing a trifluoromethyl group and  10c , bearing a triazole moiety, are potent antitumoral agents at the safe dose of 20 mg/kg against B16-F10-induced melanoma.

Synthesis, characterization and in vivo antitumor effect of new α,β-unsaturated-2,5-disubstituted-1,3,4-oxadiazoles