Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors |
| |
| Authors: | 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 |
| |
| Institution: | Chemistry Research and Discovery, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA. |
| |
| Abstract: | 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. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ |
|
