Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6220-3. doi: 10.1016/j.bmcl.2007.09.017. Epub 2007 Sep 8.

Abstract

Properly substituted pyrazolo[1,5-a]pyrimidines are potent and selective CDK2 inhibitors. Compound 15j is orally available and showed efficacy in a mouse A2780 xenograft model.

MeSH terms

  • Administration, Oral
  • Animals
  • Crystallography, X-Ray
  • Cyclin-Dependent Kinase 2 / antagonists & inhibitors*
  • Cyclin-Dependent Kinase 2 / drug effects
  • Dogs
  • Drug Screening Assays, Antitumor
  • Haplorhini
  • Mice
  • Models, Animal
  • Models, Molecular
  • Molecular Structure
  • Pyrazoles / chemical synthesis
  • Pyrazoles / chemistry*
  • Pyrazoles / pharmacology*
  • Pyridines / chemical synthesis
  • Pyridines / chemistry*
  • Pyridines / pharmacology*
  • Rats
  • Xenograft Model Antitumor Assays

Substances

  • Pyrazoles
  • Pyridines
  • pyrazolo(3,4-b)pyridine
  • Cyclin-Dependent Kinase 2

Associated data

  • PDB/2R3Q