Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects

…, I Ceballos-Picot, M Noble, J Endicott…

Index: Mettey, Yvette; Gompel, Marie; Thomas, Virginie; Garnier, Matthieu; Leost, Maryse; Ceballos-Picot, Irene; Noble, Martin; Endicott, Jane; Vierfond, Jean-Michel; Meijer, Laurent Journal of Medicinal Chemistry, 2003 , vol. 46, # 2 p. 222 - 236

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Citation Number: 145

Abstract

Cyclin-dependent kinases (CDKs) regulate the cell cycle, apoptosis, neuronal functions, transcription, and exocytosis. The observation of CDK deregulations in various pathological situations suggests that CDK inhibitors may have a therapeutic value. In this article, we report on the identification of 6-phenyl [5 H] pyrrolo [2, 3-b] pyrazines (aloisines) as a novel potent CDK inhibitory scaffold. A selectivity study performed on 26 kinases shows that ...

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