131052-61-4Relevant articles and documents
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)
Watterson, Scott H.,Langevine, Charles M.,Van Kirk, Katy,Kempson, James,Guo, Junquing,Spergel, Steven H.,Das, Jagabandhu,Moquin, Robert V.,Dyckman, Alaric J.,Nirschl, David,Gregor, Kurt,Pattoli, Mark A.,Yang, Xiaoxia,McIntyre, Kim W.,Yang, Guchen,Galella, Michael A.,Booth-Lute, Hollie,Chen, Laishun,Yang, Zheng,Wang-Iverson, David,McKinnon, Murray,Dodd, John H.,Barrish, Joel C.,Burke, James R.,Pitts, William J.
, p. 7006 - 7012 (2011)
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.
