3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation

Bioorg Med Chem Lett. 2005 May 2;15(9):2221-4. doi: 10.1016/j.bmcl.2005.03.024.

Abstract

A novel series of 2,6-diamino-3-acylpyridines were designed and synthesized as cyclin-dependent kinase (CDK) inhibitors. The representative compounds 2r and 11 showed potent CDK1 and CDK2 inhibitory activities and inhibited cellular proliferation in HeLa, HCT116, and A375 tumor cells.

MeSH terms

  • Aminopyridines / chemical synthesis*
  • Aminopyridines / pharmacology*
  • Antineoplastic Agents / pharmacology
  • Cell Division / drug effects*
  • Cell Line, Tumor
  • Cyclin-Dependent Kinases / antagonists & inhibitors*
  • Diamines / chemical synthesis*
  • Diamines / pharmacology
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • HeLa Cells
  • Humans
  • Models, Molecular
  • Molecular Conformation
  • Structure-Activity Relationship

Substances

  • Aminopyridines
  • Antineoplastic Agents
  • Diamines
  • Enzyme Inhibitors
  • Cyclin-Dependent Kinases