新型 IKK2 三环抑制剂的发现和 SAR 研究：鉴定 2-甲氧基-N-((6-(1-甲基-4-(甲氨基)-1,6-二氢咪唑并[4,5-d]吡咯并[2,3-b]吡啶-7-基)吡啶-2-基)甲基)乙酰胺（BMS-066）。
Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).
机构信息
Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA.
出版信息
Bioorg Med Chem Lett. 2011 Dec 1;21(23):7006-12. doi: 10.1016/j.bmcl.2011.09.111. Epub 2011 Oct 5.
PMID:22018461
Abstract
The synthesis, structure-activity relationships (SAR), and biological results of pyridyl-substituted azaindole based tricyclic inhibitors of IKK2 are described. Compound 4m demonstrated potent in vitro potency, acceptable pharmacokinetic and physicochemical properties, and efficacy when dosed orally in a mouse model of inflammatory bowel disease.
摘要
本文描述了基于吡啶取代的氮杂吲哚的三环 IKK2 抑制剂的合成、结构-活性关系（SAR）和生物学结果。化合物 4m 在体外具有很强的活性，在口服给予炎症性肠病小鼠模型时具有可接受的药代动力学和物理化学性质及疗效。
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