Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation

Bioorg Med Chem Lett. 2004 Dec 20;14(24):6095-9. doi: 10.1016/j.bmcl.2004.09.053.


We have identified a novel structural class of protein serine/threonine kinase inhibitors comprised of an aminoimidazo[1,2-a]pyridine nucleus. Compounds from this family are shown to potently inhibit cyclin-dependent kinases by competing with ATP for binding to a catalytic subunit of the protein. Structure-based design approach was used to direct this chemical scaffold toward generating potent and selective CDK2 inhibitors. The discovery of this new class of ATP-site directed protein kinase inhibitors, aminoimidazo[1,2-a]pyridines, provides the basis of new medicinal chemistry tool in search for an effective treatment of cancer and other diseases that involve protein kinase signaling pathways.

MeSH terms

  • Cyclin-Dependent Kinases / antagonists & inhibitors*
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Imidazoles* / chemical synthesis
  • Imidazoles* / chemistry
  • Imidazoles* / pharmacology
  • Molecular Structure
  • Pyridines* / chemical synthesis
  • Pyridines* / chemistry
  • Pyridines* / pharmacology
  • Structure-Activity Relationship


  • Enzyme Inhibitors
  • Imidazoles
  • Pyridines
  • Cyclin-Dependent Kinases