溴尿嘧啶
化学
异恶唑
体内
生物利用度
结构-活动关系
药理学
生物化学
立体化学
体外
表观遗传学
生物
遗传学
基因
作者
Jonathan T. Seal,Yann Lamotte,Frédéric Donche,Anne Bouillot,Olivier Mirguet,Françoise Gellibert,Edwige Nicodème,Gaël Krysa,Jorge Kirilovsky,Sören Beinke,Scott McCleary,Inma Rioja,Paul Bamborough,Chun‐wa Chung,Laurie Gordon,Toni Lewis,Ann L. Walker,Leanne Cutler,David Lugo,David M. Wilson,Mark Searcey,Kevin Lee,Rab K. Prinjha
标识
DOI:10.1016/j.bmcl.2012.02.041
摘要
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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