490038-59-0Relevant articles and documents
Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation
Jaramillo, Carlos,De Diego, J. Eugenio,Hamdouchi, Chafiq,Collins, Elizabeth,Keyser, Heather,Sánchez-Martínez, Concha,Del Prado, Miriam,Norman, Bryan,Brooks, Harold B.,Watkins, Scott A.,Spencer, Charles D.,Dempsey, Jack Alan,Anderson, Bryan D.,Campbell, Robert M.,Leggett, Tellie,Patel, Bharvin,Schultz, Richard M.,Espinosa, Juan,Vieth, Michal,Zhang, Faming,Timm, David E.
, p. 6095 - 6099 (2004)
Synthesis of 2-aminoimidazo[1,2-a]pyridines 1 and their evaluation as CDK2 inhibitors is described. 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.
