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)

Scott H. Watterson, 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-IversonMurray McKinnon, John H. Dodd, Joel C. Barrish, James R. Burke, William J. Pitts

Research output: Contribution to journalArticlepeer-review

6 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)7006-7012
Number of pages7
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number23
DOIs
StatePublished - Dec 1 2011

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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