Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors
| Autor: | Osslund Timothy D, Robert M. Rzasa, Ella Magal, Wenge Zhong, David Powers, Charles Henley, Jiandong Zhang, Weiya Wang, Thomas T. Nguyen, Hu Liu, Xiaoling Xiong, Matthew R. Kaller, Mark H. Norman, Hui-Ling Wang |
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| Rok vydání: | 2007 |
| Předmět: |
Models
Molecular Clinical Biochemistry Pharmaceutical Science Biochemistry Chemical synthesis Structure-Activity Relationship Cyclin-dependent kinase Drug Discovery Structure–activity relationship Enzyme Inhibitors Protein kinase A Molecular Biology Binding Sites biology Kinase Chemistry Cyclin-dependent kinase 5 Cyclin-Dependent Kinase 2 Organic Chemistry Cyclin-dependent kinase 2 Cyclin-Dependent Kinase 5 nervous system Enzyme inhibitor Drug Design Quinolines biology.protein Molecular Medicine Indicators and Reagents Protein Binding |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 17:5384-5389 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2007.07.045 |
| Popis: | 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 of quinolin-2(1H)-one derivatives. |
| Databáze: | OpenAIRE |
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