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]Pyrro Lo[2,3-B]Pyridin-7-Yl)Pyridin-2-Yl)Methyl)Acetamide (Bms-066)

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. (C) 2011 Elsevier Ltd. All rights reserved.