Dihydropyrimidones substituted pyrrole were prepared in high yields from three-component coupling of alkyl isocyanides, dialkyl acetylenedicarboxylates and dihydropyrimidone derivatives. In vitro cytotoxicity of the synthesized compounds was evaluated against HeLa cancer cell lines using MTT assay. The results shown that the cytotoxicity increased along with the increase of concentration of the compounds tested. Among these compounds, 4e and 4f including chlorine substituent displayed higher cytotoxic effect (IC50 = 10.36 ± 0.60 μM, 9.90 ± 0.20 μM), respectively, than the others tested compounds in comparison with doxorubicin (IC50 = 3.42 ± 0.20 μM) after 48 h. Also, antioxidant evaluation on the obtained products showed that the presence of substituents (electron-withdrawing or electron-donating) on the aromatic ring can play an important role in its antioxidant activity.
