2. Academic Validation
  3. 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)

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)

  • Bioorg Med Chem Lett. 2011 Dec 1;21(23):7006-12. doi: 10.1016/j.bmcl.2011.09.111.
Scott H Watterson 1,  Charles M Langevine,  Katy Van Kirk,  James Kempson,  Junquing Guo,  Steven H Spergel,  Jagabandhu Das,  Robert V Moquin,  Alaric J Dyckman,  David Nirschl,  Kurt Gregor,  Mark A Pattoli,  XiaoXia Yang,  Kim W McIntyre,  Guchen Yang,  Michael A Galella,  Hollie Booth-Lute,  Laishun Chen,  Zheng Yang,  David Wang-Iverson,  Murray McKinnon,  John H Dodd,  Joel C Barrish,  James R Burke,  William J Pitts
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-4000, USA. scott.watterson@bms.com
PMID: 22018461 DOI: 10.1016/j.bmcl.2011.09.111
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.

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