A series of novel thiazolo[3,2-a]pyrimidines were synthesized and characterized by FT-IR, 1H, 13C NMR and mass techniques. Their antioxidant activities were investigated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay and the results showed that all the synthesized compounds exhibit good antioxidant activity. In addition it was found that any substituent on the aromatic ring of the products plays an important role in their antioxidant activity. In vitro cytotoxicity of the compounds 4a-j was investigated using MTT cell viability assay. Among these compounds, 4e including chlorine substituent displayed the highest cytotoxic effect (IC50 = 6.26 ± 0.6 μM) in comparison with doxorubicin (IC50 = 0.68 ± 0.1 μM) as a standard after 72 h. Therefore, it is assumed that these compounds could be used as effective antioxidant and cytotoxic agents.
