Discovery and structure–activity relationship of coumarin derivatives as TNF-α inhibitors
| Autor: | Mi Chen, Hediki Sato, Sovouthy Tith, Yoshiyuki Ono, Hirotaka Kashiwagi, Toshiro Kozono, Akira Ishikawa, David Wallace, Thomas Arrhenius, Alex M. Nadzan, Jie-Fei Cheng, Haruhiko Sato |
|---|---|
| Rok vydání: | 2004 |
| Předmět: |
Lipopolysaccharides
Lipopolysaccharide Clinical Biochemistry Pharmaceutical Science Biochemistry Peripheral blood mononuclear cell Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Coumarins In vivo Drug Discovery Humans Structure–activity relationship Molecular Biology Cells Cultured chemistry.chemical_classification Dose-Response Relationship Drug Tumor Necrosis Factor-alpha Organic Chemistry Coumarin In vitro chemistry Leukocytes Mononuclear Molecular Medicine Tumor necrosis factor alpha Lactone |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 14:2411-2415 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2004.03.022 |
| Popis: | The discovery and structure–activity relationship of a novel series of coumarin-based TNF-α inhibitors is described. Starting from the initial lead 1a , various derivatives were prepared surrounding the coumarin core structure to optimize the in vitro inhibitory activity of TNF-α production by human peripheral blood mononuclear cells (hPBMC), stimulated by bacterial lipopolysaccharide (LPS). Selected compounds also demonstrated in vivo inhibition of TNF-α production in rats. |
| Databáze: | OpenAIRE |
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