Cyclin dependent kinase (CDK) inhibitors as anticancer drugs

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3420-35. doi: 10.1016/j.bmcl.2015.05.100. Epub 2015 Jun 6.


Sustained proliferative capacity is a hallmark of cancer. In mammalian cells proliferation is controlled by the cell cycle, where cyclin-dependent kinases (CDKs) regulate critical checkpoints. CDK4 and CDK6 are considered highly validated anticancer drug targets due to their essential role regulating cell cycle progression at the G1 restriction point. This review provides an overview of recent advances on cyclin dependent kinase inhibitors in general with special emphasis on CDK4 and CDK6 inhibitors and compounds under clinical evaluation. Chemical structures, structure activity relationships, and relevant preclinical properties will be described.

Keywords: CDK inhibitors; Cell cycle.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Cell Cycle
  • Cyclin-Dependent Kinase Inhibitor Proteins / metabolism*
  • Humans
  • Neoplasms / drug therapy*


  • Antineoplastic Agents
  • Cyclin-Dependent Kinase Inhibitor Proteins