Imidazo[1,2-a]pyridines. Part 2: SAR and optimisation of a potent and selective class of cyclin-dependent kinase inhibitors

Bioorg Med Chem Lett. 2004 May 3;14(9):2245-8. doi: 10.1016/j.bmcl.2004.02.015.


Exploration of SAR and optimisation of the imidazo[1,2-a]pyridine CDK inhibitors has lead to the discovery of novel, potent and selective inhibitors of the cyclin-dependent kinase CDK2. Understanding of SAR has identified positions of substitution, which allow modification of physical properties and offer the potential for in vivo optimisation.

MeSH terms

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


  • Enzyme Inhibitors
  • Pyridines
  • Cyclin-Dependent Kinases