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CDKs are members of serine/threonine kinase family and key enzymes in cell cycle progression and transcription and other major biological processes including neural differentiation and metabolism. Constitutive or deregulated hyperactivity of these kinases due to amplification, over expression or mutation of cyclins or CDK, contributes to proliferation of cancer cells, and irregular activity of these kinases has been reported in a wide variety of human cancers. Therefore, CDKs considered as attractive pharmacological targets for development of anticancer therapeutics. This book first summarizes the different functions of CDKs and the biological structure of CDKs, cell cycle and their role in cell cycle regulation. Then it focuses on CDKs inhibitors as anticancer and the different strategies in developing it, CDK2 inhibitors that inter clinical trials and CDK4/6 inhibitors that in the way of approval have been discussed. Future perspective of CDKs inhibitors as anticancer will be defined in the development of new target CDK1, CDK5, CDK7, CDK8, CDK9 and CDK12 inhibitors.