Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374627 | Bioorganic & Medicinal Chemistry Letters | 2010 | 6 Pages |
Abstract
A series of acyloxyalkyl and amidooxyalkyl ketones appended to a carbobenzyloxy aspartic acid core have been prepared. The most potent of these new inhibitors was 4i with a Ki of 0.5 μM. These two series provide an improved understanding of the binding requirements for the hydrophobic prime side of ICE.
Graphical abstractAcyloxyalkyl, 4, and amidooxyalkyl, 7, ketones based on aspartic acid have been prepared. These two series provide an improved understanding of the binding requirements for the hydrophobic prime side of ICE.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Paul Galatsis, Bradley Caprathe, Dennis Downing, John Gilmore, William Harter, Sheryl Hays, Catherine Kostlan, Kristin Linn, Elizabeth Lunney, Kim Para, Anthony Thomas, Joseph Warmus, Hamish Allen, Kenneth Brady, Robert Talanian, Nigel Walker,