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A novel Pd-catalyzed cyclization reaction of ureas for the synthesis of dihydroquinazolinone p38 kinase inhibitors.

Schlapbach, Achim and 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

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

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