Novel tricyclic inhibitors of 1κB kinase

James Kempson, Steven H. Spergel, Junqing Guo, Claude Quesnelle, Patrice Gill, Dominique Belanger, Alaric J. Dyckman, Tianle Li, Scott H. Watterson, Charles M. Langevine, Jagabandhu Das, Robert V. Moquin, Joseph A. Furch, Anne Marinier, Marco Dodier, Alain Martel, David Nirschl, Katy Van Kirk, James R. Burke, Mark A. PattoliKathleen Gillooly, Kim W. McIntyre, Chen Laishun, Yang Zheng, Punit H. Marathe, David Wang-Iverson, John H. Dodd, Murray McKinnon, Joel C. Barrish, William J. Pitts

Research output: Contribution to journalArticlepeer-review

29 Scopus citations


The design and synthesis of a novel series of oxazole-, thiazole-, and imidazole-based inhibitors of IκB kinase (IKK) are reported. Biological activity was improved compared to the pyrazolopurine lead, and the expedient synthesis of the new tricyclic systems allowed for efficient exploration of structure-activity relationships. This, combined with an iterative rat cassette dosing strategy, was used to identify compounds with improved pharmacokinetic (PK) profiles to advance for in vivo evaluation.

Original languageEnglish (US)
Pages (from-to)1994-2005
Number of pages12
JournalJournal of Medicinal Chemistry
Issue number7
StatePublished - Apr 9 2009

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery


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