Journal of Medicinal Chemistry p. 1994 - 2005 (2009)
Update date:2022-09-26
Topics:
Kempson, James
Spergel, Steven H.
Guo, Junqing
Quesnelle, Claude
Gill, Patrice
Belanger, Dominique
Dyckman, Alaric J.
Li, Tianle
Watterson, Scott H.
Langevine, Charles M.
Das, Jagabandhu
Moquin, Robert V.
Furch, Joseph A.
Marinier, Anne
Dodier, Marco
Martel, Alain
Nirschl, David
Van Kirk, Katy
Burke, James R.
Pattoli, Mark A.
Gillooly, Kathleen
McIntyre, Kim W.
Laishun, Chen
Zheng, Yang
Marathe, Punit H.
Wang-Iverson, David
Dodd, John H.
McKinnon, Murray
Barrish, Joel C.
Pitts, William J.
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.
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