Design and synthesis of marine fungal phthalide derivatives as PPAR-γ agonists
| Autor: | Jian Lin Li, Bin Xiao, Hae Young Chung, Minhi Park, Juan Liu, Jongki Hong, Jun Yin, Eun La Kim, Jee H. Jung |
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| Rok vydání: | 2012 |
| Předmět: |
Models
Molecular Stereochemistry Clinical Biochemistry Pharmaceutical Science Peroxisome proliferator-activated receptor Binding Competitive Biochemistry Cell Line Phthalide chemistry.chemical_compound Drug Discovery medicine Animals Luciferase Molecular Biology Benzofurans chemistry.chemical_classification Molecular Structure Ligand binding assay Organic Chemistry Peroxisome Rats PPAR gamma Liver chemistry Docking (molecular) Drug Design Molecular Medicine Rosiglitazone Binding domain medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry. 20:4954-4961 |
| ISSN: | 0968-0896 |
| Popis: | On the basis of a marine fungal phthalide (paecilocin A) skeleton, we synthesized 20 analogs and evaluated them for peroxisome proliferator-activated receptor gamma (PPAR-γ) binding and activation. Among these analogs, 6 and 7 had significant PPAR-γ binding activity, and 7 showed further PPAR-γ activation in rat liver Ac2F cells. In docking simulation, 7 formed H bonds with key amino acid residues of the PPAR-γ binding domain, and the overall positioning was similar to rosiglitazone. This new phthalide derivative is considered an interesting new molecular class of PPAR-γ ligands. |
| Databáze: | OpenAIRE |
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