Identification of selective inhibitors of cyclin dependent kinase 4

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2209-11. doi: 10.1016/s0960-894x(01)00416-4.

Abstract

A new structural type of kinase inhibitor, containing a benzocarbazole nucleus, has been identified. Members of the series are selective for inhibition of the cyclin dependent kinase family of enzymes. Although the cdks are highly homologous, representatives of the series showed intra-cdk selectivities, especially for cdk4. SAR studies elucidated the important features of the molecules for inhibition.

MeSH terms

  • Carbazoles / chemistry
  • Carbazoles / pharmacology*
  • Cyclin-Dependent Kinase 4
  • Cyclin-Dependent Kinases / antagonists & inhibitors*
  • Cyclin-Dependent Kinases / metabolism
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Molecular Conformation
  • Proto-Oncogene Proteins*
  • Structure-Activity Relationship

Substances

  • Carbazoles
  • Enzyme Inhibitors
  • Proto-Oncogene Proteins
  • Cyclin-Dependent Kinase 4
  • Cyclin-Dependent Kinases