The material basis for the development and progression of malignant tumors is the biosynthesis of nucleic acids and proteins. In the process of synthesis, nucleotides are formed from their precursors and thereafter polymerized in a certain order to form nucleic acids. From the point of view of molecular biology, DNA is considered as a template, which is used to form messenger RNA (mRNA) and various transfer RNAs (tRNA) that work together to synthesize proteins from amino acids on nucleoprotein bodies. At the same time, certain enzymes are responsible for the synthesis of DNA and nucleotides, which is the target of antitumor drugs. Clinically used antitumor drugs: 1. Drugs that directly damage DNA and prevent its replication: such as alkylating agents, some antibiotics, platinum, etc. The site of action of these drugs is DNA. The action site of such drugs is DNA, which mainly affects the deconvolution and replication of DNA, and at the same time can make DNA single or double strand break, so that its cell division cannot be carried out to control the occurrence and development of tumor. 2. Drugs that affect the biosynthesis of nucleic acid (DNA, RNA): such as anti-metabolic drugs: methotrexate, fluorouracil, cytarabine, etc. It mainly affects the enzymatic system of tumor cells, blocking the synthesis of DNA or RNA precursors, and finally reaching the barrier of DNA or RNA formation, affecting nucleic acid biosynthesis, causing inhibition of tumor cell growth and reproduction, and prompting apoptosis. 3. Drugs that act on nucleic acid transcription: such as antibiotics: actinomycin-D, aclarubicin, etc. Selective action on DNA template, inhibition of DNA-dependent RNA polymutase, affecting RNA synthesis.4. Drugs affecting microtubule protein synthesis: such as plant-based drugs: paclitaxel, vincristine, onychomycin. They mainly affect mitosis and stop the process of its proliferative phase.5. Other classes of drugs: such as biological response modifiers, which can enhance the host’s anti-tumor response, enhance the host’s tolerance to cytotoxic substances, change the cell membrane structure, enhance immunogenicity, and prevent its cellular transformation. Targeted therapeutic drugs take the change of tumor cell characteristics as the target of action, and reduce the toxic reaction to normal cells while exerting anti-tumor activity.