Protein kinase inhibitors from the urea class.
Protein kinase inhibitors hold great potential as novel therapies for cancer and inflammatory disorders. While bis-aryl ureas have been reported as kinase inhibitors as early as 1996, a number of publications and patent applications appeared in the literature during the past two years. Three urea-based kinase inhibitors are currently undergoing clinical trials. The present review summarizes available data, and provides an overview of the structure-activity relationships against a variety of kinase targets, including p38, Raf-1 and cyclin-dependent kinases.
Dumas
Jacques
J
Bayer Research Center, Bayer Corporation, Pharmaceutical Division, 400 Morgan Lane, West Haven, CT 06516, USA. jacques.dumas.b@bayer.com
D000818:Animals; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors; D004345:Drug Industry; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D020928:Mitogen-Activated Protein Kinases / Q000037:antagonists & inhibitors; D047428:Protein Kinase Inhibitors; D014508:Urea / Q000737:chemistry* / Q000494:pharmacology*; D048051:p38 Mitogen-Activated Protein Kinases
D004791:Enzyme Inhibitors; D047428:Protein Kinase Inhibitors; D014508:Urea; D018844:Cyclin-Dependent Kinases; D020928:Mitogen-Activated Protein Kinases; D048051:p38 Mitogen-Activated Protein Kinases