التفاصيل البيبلوغرافية
العنوان:
Novel Tricyclic Inhibitors of IκB Kinase
المؤلفون:
Charles M. Langevine , Joseph A. Furch , Dominique Belanger , Mark A. Pattoli , Joel C. Barrish , Alaric J. Dyckman , Marco Dodier , James Kempson , Jagabandhu Das , David S. Nirschl , Laishun Chen , Punit Marathe , Kathleen M. Gillooly , Junqing Guo , Robert V. Moquin , John H. Dodd , Murray McKinnon , Anne Marinier , Zheng Yang , Steven H. Spergel , Claude A. Quesnelle , Kim W. McIntyre , Katy Van Kirk , James R. Burke , William J. Pitts , Scott H. Watterson , Alain Martel , Patrice Gill , David B. Wang-Iverson , Tianle Li
المصدر:
Journal of Medicinal Chemistry . 52:1994-2005
بيانات النشر:
American Chemical Society (ACS), 2009.
سنة النشر:
2009
مصطلحات موضوعية:
Lipopolysaccharides , Recombinant Fusion Proteins , IκB kinase , In Vitro Techniques , Crystallography, X-Ray , Chemical synthesis , Mice , Structure-Activity Relationship , chemistry.chemical_compound , Drug Discovery , Animals , Humans , Thiazole , Oxazoles , Glutathione Transferase , Oxazole , chemistry.chemical_classification , Mice, Inbred BALB C , Tumor Necrosis Factor-alpha , Imidazoles , Biological activity , I-kappa B Kinase , Rats , Thiazoles , Enzyme , chemistry , Biochemistry , Leukocytes, Mononuclear , Microsomes, Liver , Molecular Medicine , Female , Signal transduction , Heterocyclic Compounds, 3-Ring , Tricyclic
الوصف:
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.
تدمد:
1520-4804
URL الوصول:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f4567117bd8910f92df6183547c38087 https://doi.org/10.1021/jm8015816
رقم الأكسشن:
edsair.doi.dedup.....f4567117bd8910f92df6183547c38087
قاعدة البيانات:
OpenAIRE
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