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  • Title: Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation.
    Author: Jaramillo C, de Diego JE, Hamdouchi C, Collins E, Keyser H, Sánchez-Martínez C, del Prado M, Norman B, Brooks HB, Watkins SA, Spencer CD, Dempsey JA, Anderson BD, Campbell RM, Leggett T, Patel B, Schultz RM, Espinosa J, Vieth M, Zhang F, Timm DE.
    Journal: Bioorg Med Chem Lett; 2004 Dec 20; 14(24):6095-9. PubMed ID: 15546737.
    Abstract:
    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.
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