2. Academic Validation
  3. Novel tricyclic inhibitors of IkappaB kinase

Novel tricyclic inhibitors of IkappaB kinase

  • J Med Chem. 2009 Apr 9;52(7):1994-2005. doi: 10.1021/jm8015816.
James Kempson 1,  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 Pattoli,  Kathleen Gillooly,  Kim W McIntyre,  Laishun Chen,  Zheng Yang,  Punit H Marathe,  David Wang-Iverson,  John H Dodd,  Murray McKinnon,  Joel C Barrish,  William J Pitts
Affiliations

Affiliation

  • 1 Departments of Discovery Chemistry, Discovery Biology, and Metabolism and Pharmacokinetics and Synthesis and Analysis Technology Team, Bristol-Myers Squibb Research and Development, Princeton, New Jersey 08543-4000, USA.
PMID: 19267461 DOI: 10.1021/jm8015816
Abstract

The design and synthesis of a novel series of oxazole-, thiazole-, and imidazole-based inhibitors of IkappaB 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.

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