Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation |
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Authors: | 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 |
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Institution: | Centro de Investigación Lilly, Avenida de la Industria, 30, 28108 Alcobendas, Madrid, Spain. |
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Abstract: | We have identified a novel structural class of protein serine/threonine kinase inhibitors comprised of an aminoimidazo1,2-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, aminoimidazo1,2-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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Keywords: | Cyclin-dependent kinase CDK Imidazopyridine Kinase |
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