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Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1

…, Y Ferandin, L Demange, A Lopez-Giral…

文献索引:Oumata, Nassima; Bettayeb, Karima; Ferandin, Yoan; Demange, Luc; Lopez-Giral, Angela; Goddard, Marie-Lorene; Myrianthopoulos, Vassilios; Mikros, Emmanuel; Flajolet, Marc; Greengard, Paul; Meijer, Laurent; Galons, Herve Journal of Medicinal Chemistry, 2008 , vol. 51, # 17 p. 5229 - 5242

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被引用次数: 102

摘要

Cyclin-dependent kinases (CDKs) and casein kinases 1 (CK1) are involved in the two key molecular features of Alzheimer's disease, production of amyloid-β peptides (extracellular plaques) and hyper-phosphorylation of Tau (intracellular neurofibrillary tangles). A series of 2, 6, 9-trisubstituted purines, structurally related to the CDK inhibitor roscovitine, have been synthesized. They mainly differ by the substituent on the C-6 position. These compounds ...