Aurora kinase is a family of serine/threonine protein kinases and plays essential roles in cell proliferation. The human Aurora kinase family has three members: Aurora A, Aurora B and Aurora C. Aurora family kinase has critical roles in mitotic progression. Aberrant expression of Aurora kinase causes abnormal mitotic progression and thereby leads to genetic instability and carcinogenesis. Aurora kinase is frequently over-expressed in many types of human tumors and contributes to the tumors development. Thus, development of inhibitors targeting Aurora family kinase provides new strategies for cancer treatment. To date, a considerable number of Aurora family kinase inhibitors have been developed, among which, great antitumor effects were shown in some inhibitors and progressed into clinical studies.