Genistein has a variety of biological activities, such as estrogen, anti-tumor, prevent osteoporosis, anti-oxidation, lipid-reduction, anti-atherosclerosis and other physical activity. It has become a hot spot for worldwide in recent years. This review focuses on the anti-tumor activity of genistein derivatives, in order to facilitate its research and applications, and provide the basis for molecular design for the purpose of anti-tumor prodrug.