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.

Concepción Sánchez-Martínez ¹, Lawrence M Gelbert ², María José Lallena ³, Alfonso de Dios ⁴

Affiliations

1 Discovery Chemistry Research and Technologies, Eli Lilly and Company, Alcobendas (Madrid) 28108, Spain. Electronic address: sanchez-martinez_concepcion@lilly.com.
2 Herman B Wells Center for Pediatric Research, Section of Pediatric Hematology, Oncology, Indiana University, Indianapolis, IN 46202, United States.
3 Discovery Chemistry Research and Technologies, Eli Lilly and Company, Alcobendas (Madrid) 28108, Spain.
4 Discovery Chemistry Research and Technologies, Eli Lilly and Company, Indianapolis, IN 46285, United States.

PMID: 26115571 DOI: 10.1016/j.bmcl.2015.05.100

Abstract

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.

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