Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 7, Pages 1994-2005Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm8015816
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The design and synthesis of a novel series of oxazole-, thiazole-, and imidazole-based inhibitors of I kappa B 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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