Design and synthesis of quinolin-2 (1H)-one derivatives as potent CDK5 inhibitors

…, E Magal, T Nguyen, TD Osslund, D Powers…

文献索引：Zhong, Wenge; Liu, Hu; Kaller, Matthew R.; Henley, Charles; Magal, Ella; Nguyen, Thomas; Osslund, Timothy D.; Powers, David; Rzasa, Robert M.; Wang, Hui-Ling; Wang, Weiya; Xiong, Xiaoling; Zhang, Jiandong; Norman, Mark H. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 19 p. 5384 - 5389

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被引用次数: 20

摘要

Cyclin-dependent kinase 5 (CDK5) is a serine/threonine protein kinase and its deregulation is implicated in a number of neurodegenerative disorders such as Alzheimer's disease, amyotrophic lateral sclerosis, and ischemic stroke. Using active site homology modeling between CDK5 and CDK2, we explored several different chemical series of potent CDK5 inhibitors. In this report, we describe the design, synthesis, and CDK5 inhibitory activities ...