Abstract: OBJECTIVE To explore the novel antineoplastic drugs by screening the monophenolic derivatives with high antioxidant activity. METHODS According to the literature in recent years, monophenolic antioxidants and their derivatives were discussed about the clinical research and mechanism. RESULTS The derivatives of monophenolic antioxidant were more stable or more effective than monophenolic antioxidant in antineoplastic activity. CONCLUSION As the research of the structure-activity relationship moves along, it will be possible to provide more safe and effective drugs for clinical through the modification of monophenolic antioxidants.