A novel Pd-catalyzed cyclization reaction of ureas for the synthesis of dihydroquinazolinone p38 kinase inhibitors.
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Schlapbach, Achim, Heng, Richard and Di Padova, Franco E. (2004) A novel Pd-catalyzed cyclization reaction of ureas for the synthesis of dihydroquinazolinone p38 kinase inhibitors. Bioorganic & Medicinal Chemistry Letters, 14 (2). pp. 357-360. ISSN 0960-894X
Official URL: http://www.sciencedirect.com/science?_ob=ArticleUR...
Abstract
A series of potent p38 inhibitors based on the dihydroquinazoline scaffold was synthesized using a novel Pd-catalyzed cyclization reaction of aryl-benzyl ureas. Optimization of this compound class led to compound 20, which inhibits p38alpha in vitro with IC(50)=14 nM and is active in the mouse TNFalpha-release model.
Item Type: | Article |
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Additional Information: | author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used |
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Date Deposited: | 14 Dec 2009 14:01 |
Last Modified: | 31 Jan 2013 01:19 |
URI: | https://oak.novartis.com/id/eprint/327 |