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).

Published

Journal Article

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.

Full Text

Duke Authors

Cited Authors

  • Watterson, SH; Langevine, CM; Van Kirk, K; Kempson, J; Guo, J; Spergel, SH; Das, J; Moquin, RV; Dyckman, AJ; Nirschl, D; Gregor, K; Pattoli, MA; Yang, X; McIntyre, KW; Yang, G; Galella, MA; Booth-Lute, H; Chen, L; Yang, Z; Wang-Iverson, D; McKinnon, M; Dodd, JH; Barrish, JC; Burke, JR; Pitts, WJ

Published Date

  • December 1, 2011

Published In

Volume / Issue

  • 21 / 23

Start / End Page

  • 7006 - 7012

PubMed ID

  • 22018461

Pubmed Central ID

  • 22018461

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2011.09.111

Language

  • eng

Conference Location

  • England