Design and synthesis of 6-oxo-1, 6-dihydropyridines as CDK5 inhibitors

…, C Henley, E Magal, T Nguyen, D Powers…

Index: Kaller, Matthew R.; Zhong, Wenge; Henley, Charles; Magal, Ella; Nguyen, Thomas; Powers, David; Rzasa, Robert M.; Wang, Weiya; Xiong, Xiaoling; Norman, Mark H. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 23 p. 6591 - 6594

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Citation Number: 6

Abstract

Cyclin-dependent kinase 5 (CDK5) is a serine-threonine protein kinase that plays a significant role in neuronal development. In association with p25, CDK5 abnormally phosphorylates a number of cellular targets involved in neurodegenerative disorders. Using active site homology and previous structure–activity relationships, a new series of potent CDK5 inhibitors was designed. This report describes the optimization of 6-oxo-1, 6- ...