Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371880 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
In this Letter we report the synthesis and evaluation of a series of non-amidine inhibitors of Urokinase Plasminogen Activator (uPA). Starting from compound 1, a significant change provided compounds in which the amidine, binding in the S1 pocket, was replaced with a primary amine. Further modifications led to the identification of potent, selective, and orally bioavailable uPA inhibitors.
Graphical abstractThe discovery, synthesis, and early SAR work on a benzyl amine containing series of uPA inhibitors is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Christopher W. West, Marc Adler, Danny Arnaiz, Deborah Chen, Kieu Chu, Giovanna Gualtieri, Elena Ho, Christoph Huwe, David Light, Gary Phillips, Rebecca Pulk, Drew Sukovich, Marc Whitlow, Shendong Yuan, Judi Bryant,