| Literature DB >> 22437115 |
Jonathan Seal1, 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, Ann L Walker, Leanne Cutler, David Lugo, David M Wilson, Jason Witherington, Kevin Lee, Rab K Prinjha.
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.Entities:
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Year: 2012 PMID： 22437115 DOI： 10.1016/j.bmcl.2012.02.041
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823