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2005
Enzyme inhibiting activity
X 0220
Aminoimidazo[1,2-a]pyridines as a New Structural Class of Cyclin-Dependent KiInhibitors. Part 1. Design, Synthesis, and Biological Evaluation. — A struc16- 223 nase
ture-based design approach is used to disclose a structure—activity—relationship study
of aminoimidazo[1,2-a]pyridines around substituents 3 and 6 of the aromatic
bicyclic nucleus. The members of this structural class potently inhibit either CDK1 or
CDK2 by competing with ATP for binding to a catalytic subunit of the protein. All compounds display less activity against CDK4 than against either CDK1 or CDK2. Compounds (I), (II), and (III) are selective for CDK1 vs. CDK2, while CDK2 vs. CDK1
selectivity is achieved with (IV) and (V). This new class provides a new
medicinal chemistry tool in the search for an effective treatment of cancer and diseases
that involve protein kinase signaling pathways. — (JARAMILLO*, C.; et al.; Bioorg.
Med. Chem. Lett. 14 (2004) 24, 6095-6099; Cent. Invest. Lilly SA,
E-28108 Alcobendas, Madrid, Spain; Eng.) — H. Hoennerscheid
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