6533b7d1fe1ef96bd125c245
RESEARCH PRODUCT
Synthesis and evaluation of diverse thio avarol derivatives as potential UVB photoprotective candidates.
Miguel PayáMaría Carmen TerencioMaria AmigóSalvatore De RosaCarmine Iodicesubject
AntioxidantMagnetic Resonance SpectroscopyNeutrophilsPhotochemistryUltraviolet Raysmedicine.medical_treatmentChemistry PharmaceuticalClinical BiochemistryMolecular ConformationPharmaceutical ScienceThio-BiochemistryChemical synthesisAntioxidantsCell Line TumorDrug DiscoverymedicineHumansCytotoxicityMolecular Biologyintegumentary systemChemistryTumor Necrosis Factor-alphaOrganic ChemistryNF-kappa BSemisynthesisIn vitroHaCaTmedicine.anatomical_structureBiochemistryModels ChemicalDrug DesignMolecular MedicineKeratinocyteReactive Oxygen SpeciesSesquiterpenesdescription
Semisynthesis of 13 new thio avarol derivatives (4-16) and in vitro evaluation on the photodamage response induced by UVB irradiation are described. Their ability to inhibit NF-kappaB activation and TNF-alpha generation in HaCaT cells as well as their antioxidant capacity in human neutrophils has also been studied. Among them we have identified two monophenyl thio avarol derivatives (4-5) lacking cytotoxicity which can be considered promising UVB photoprotective agents through the potent inhibition of NF-kappaB activation with a mild antioxidant pharmacological profile.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2007-05-01 | Bioorganicmedicinal chemistry letters |