Author/Authors :
Wenge Zhong، نويسنده , , Hu Liu، نويسنده , , Matthew R. Kaller، نويسنده , , Charles Henley، نويسنده , , Ella Magal، نويسنده , , Thomas Nguyen، نويسنده , , Timothy D. Osslund، نويسنده , , David Powers، نويسنده , , Robert M. Rzasa، نويسنده , , Hui-Ling Wang، نويسنده , , Weiya Wang، نويسنده , , Xiaoling Xiong، نويسنده , , Jiandong Zhang، نويسنده , , Mark H. Norman، نويسنده ,
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 :
kinase , Neurodegenerative disorders , CDK5 inhibitor , quinolin-2(1H)-one
