Design, synthesis and SAR of phenylamino-substituted 5,11-dihydro-dibenzo[a,d]cyclohepten-10-ones and 11H-dibenzo[b,f]oxepin-10-ones as p38 MAP kinase inhibitors
| Autor: | Angelika Dorn, Stefan Laufer, Verena Schattel |
|---|---|
| Rok vydání: | 2010 |
| Předmět: |
Stereochemistry
p38 mitogen-activated protein kinases Interleukin-1beta Clinical Biochemistry Anti-Inflammatory Agents Pharmaceutical Science p38 Mitogen-Activated Protein Kinases Biochemistry Chemical synthesis Proinflammatory cytokine Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Structure–activity relationship Computer Simulation heterocyclic compounds Cycloheptanes Protein Kinase Inhibitors Molecular Biology Binding Sites biology Tumor Necrosis Factor-alpha Chemistry Organic Chemistry Small molecule Enzyme inhibitor Drug Design Mitogen-activated protein kinase Oxepins biology.protein Lactam Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 20:3074-3077 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2010.03.107 |
| Popis: | The p38 MAP kinase is a key enzyme in inflammatory diseases as it is involved in the biosynthesis of proinflammatory cytokines such as TNF-alpha and IL-1beta. Small molecule p38 inhibitors suppress the production of these cytokines and therefore p38 is a promising drug target for novel anti-inflammatory therapeutics. In this study, we report the design, synthesis, and SAR of novel N-substituted 11H-dibenzo[b,f]oxepin-10-ones and 5,11-dihydro-dibenzo[a,d]cyclohepten-10-ones as p38 inhibitors. |
| Databáze: | OpenAIRE |
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