This review article displays some new proteins in cell cycle, such as Cyclin /CDK complex, polo-like kinases (PLKs), Aurora kinases and Kinesins spindle protein (KSP). These new proteins are the new targets for new antitumor agent development. Many researches found that compounds could inhibit these new targets would show good growth inhibition activity against human tumor cell lines and avoid the side effect of chemotherapy by the traditional antitumor drugs. We believe that the information disclosed in this article will be a new current for the development of new anticancer drugs.