Synthesis of 4‐Hydroxy‐2‐pyridinone Derivatives and Evaluation of Their Antioxidant/Anticancer Activities

Abstract A simple approach was applied for the regioselective synthesis of various pyridine‐2‐one derivatives or annulated pyridine as novel heterocyclic systems from the reaction of dehydroacetic acid (DHA) with mono‐ or bidentate nucleophile as with benzylamine and/or phenylenediamines in dichloromethane followed by transformation with different halo‐compounds in refluxing 1,4‐dioxane has been achieved in moderate to excellent yields (48‐93 %). In addition, DFT studies of the key synthesized compounds were carried out for confirmed proposed mechanisms. The newly synthesized compounds were screened for their in‐vitro inhibition activities against mammary gland breast cancer (MCF‐7) and human prostate cancer (PC‐3) using the MTT colorimetric method. Also, the target synthesized compounds were evaluated as antioxidant agents.