At present, amino acid derivatives have been widely used as anti-tumor drugs. The application forms are: (1) as the carrier of anti-tumor drugs to increase the solubility of drugs, such as: phenylalanine mustard qi, L-cypamine, L-L-L-L– Corticine, L-lysine, and phenylramine nitrogen mustard are binding; (2) the structural analogy of amino acids required for tumor cells to inhibit cell proliferation, such as: S-ammonia-L-cysteine ammonia Acid; (3) As an enzyme inhibitor, the synthesis path of interrupt pyrimidine nucleic acid, such as: N-phosphate acetyl -l-Tianmen citrium is a transitional inhibitor of a gatemic acid rotorphenols; (4) As an amino acid derivatives that make cancer cells reverse, they improve their targetedness to tumor cells. As an endogenous substance of life, it can introduce it to drug molecules, which can promote the absorption of drugs by cells, reduce the toxicity of the drug, and open up ways to seek efficient and low -toxic antitumor drugs.