HDACs and HATs are two kinds of enzymes which catalyse deacetylation and acetylation of histone in eukaryotes, whose dynamic balance has accurate regulation for gene transcription and gene expression of eukaryotes at DNA level. Disbalance of them can bring the disorder of proliferation and differentiation in normal cells, and then lead to the initiation of tumor. Their aberrant functions were directly related to the initiation and progression of various tumors, such as promyelocytic leukemia, Hodgkin lymphoma, colonic cancer and gastral cancer. The inhibitors of HDACs are used for treatment of tumor. They can restrain the activity of HDACs and block the inhibition of gene expression caused by the disorder of deacetylation. Its major biological effects lie in inducing differentiation of tumor cells, arresting cell circle at G0/G1, activating cell apoptosis gene, enhancing the sensitivity of chemical therapy and radioactive therapy. So far HDAC has been an important target enzyme in anticancer drug research.