Structure–activity relationships of 3, 4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors

…, TT Nguyen, TD Osslund, D Powers, VJ Santora…

Index: Rzasa, Robert M.; Kaller, Matthew R.; Liu, Gang; Magal, Ella; Nguyen, Thomas T.; Osslund, Timothy D.; Powers, David; Santora, Vincent J.; Viswanadhan, Vellarkad N.; Wang, Hui-Ling; Xiong, Xiaoling; Zhong, Wenge; Norman, Mark H. Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 20 p. 6574 - 6595

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Citation Number: 33

Abstract

Cyclin-dependent kinase 5 (CDK5) is a serine/threonine kinase that plays a critical role in the early development of the nervous system. Deregulation of CDK5 is believed to contribute to the abnormal phosphorylation of various cellular substrates associated with neurodegenerative disorders such as Alzheimer's disease, amyotrophic lateral sclerosis, and ischemic stroke. Acyclic urea 3 was identified as a potent CDK5 inhibitor and co- ...