The invention belongs to the technical field of 
medicinal chemistry, and particularly relates to a tetravalent 
platinum naphthalimide complex, a preparation method and application thereof. The tetravalent 
platinum naphthalimide complex has good anti-tumor activity, which is better than that of cis-
platinum and 
oxaliplatin, and the tetravalent platinum naphthalimide complex has better stability than bivalent platinum like cis-platinum, 
carboplatin and 
oxaliplatin. According to the invention, the naphthalimide modified tetravalent platinum has good targeting performance on 
tumor cells, 
high selectivity on 
tumor cells is improved, and different from a classic 
divalent platinum 
drug, the complex provided by the invention regulates and controls subcellular organelles and 
cell nucleus functionsto reverse 
drug resistance by targeting a tumor high 
polyamine microenvironment, and relieves 
immunosuppression of T cells around tumors at the same time. The complex provided by the invention also solves the problems of poor 
solubility, tedious clinical compatibility, poor patient 
immunity in clinical application of 
chemotherapeutic drugs and the like of previous bivalent platinum antitumor drugs, and has good 
fat solubility and water 
solubility.