| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1361313 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
A novel series of quinoline isoxazole BET family bromodomain inhibitors are discussed. Crystallography is used to illustrate binding modes and rationalize their SAR. One member, I-BET151 (GSK1210151A), shows good oral bioavailability in both the rat and minipig as well as demonstrating efficient suppression of bacterial induced inflammation and sepsis in a murine in vivo endotoxaemia model.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jonathan Seal, Yann Lamotte, Frédéric Donche, Anne Bouillot, Olivier Mirguet, Françoise Gellibert, Edwige Nicodeme, Gael Krysa, Jorge Kirilovsky, Soren Beinke, Scott McCleary, Inma Rioja, Paul Bamborough, Chun-Wa Chung, Laurie Gordon, Toni Lewis,