| 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. | |
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MedLine Citation:
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PMID: 20418099 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Angelika Dorn; Verena Schattel; Stefan Laufer |
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Publication Detail:
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Type: Journal Article Date: 2010-04-01 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 20 ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2010 May |
Date Detail:
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Created Date: 2010-05-04 Completed Date: 2010-08-02 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 3074-7 Citation Subset: IM |
Copyright Information:
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Copyright 2010 Elsevier Ltd. All rights reserved. |
Affiliation:
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Institute of Pharmacy, Department of Pharmaceutical and Medicinal Chemistry, Eberhard-Karls-University Tübingen, 72076 Tübingen, Germany. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Anti-Inflammatory Agents Binding Sites Computer Simulation Cycloheptanes / chemical synthesis, chemistry*, pharmacology Drug Design Interleukin-1beta / metabolism Oxepins / chemical synthesis, chemistry*, pharmacology Protein Kinase Inhibitors / chemical synthesis, chemistry*, pharmacology Structure-Activity Relationship Tumor Necrosis Factor-alpha / metabolism p38 Mitogen-Activated Protein Kinases / antagonists & inhibitors*, metabolism |
| Chemical | |
Reg. No./Substance:
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0/Anti-Inflammatory Agents; 0/Cycloheptanes; 0/Interleukin-1beta; 0/Oxepins; 0/Protein Kinase Inhibitors; 0/Tumor Necrosis Factor-alpha; EC 2.7.11.24/p38 Mitogen-Activated Protein Kinases |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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