| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371375 | Bioorganic & Medicinal Chemistry Letters | 2010 | 7 Pages |
Abstract
By targeting an extended region of the conventional ‘DFG-out’ pocket of p38α, while minimizing interactions with the specificity pocket and eliminating interactions with the adenine binding site, we are able to design and synthesize a number of pyrazole-urea based DFG-out p38α inhibitors with good potencies, and excellent selectivity.
Graphical abstractThe development of potent and selective p38 inhibitor 11 is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Hu Liu, Cyrille Kuhn, Frederic Feru, Suzanne L. Jacques, Gayatri D. Deshmukh, Ping Ye, Glen R. Rennie, Theresa Johnson, Steven Kazmirski, Simon Low, Rocco Coli, Yuan-hua Ding, Alan C. Cheng, Haile Tecle, Jessie M. English, Robert Stanton, Joe C. Wu,