Synthesis and evaluation of diverse thio avarol derivatives as potential UVB photoprotective candidates

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-κB activation and TNF-α generation in HaCaT cells as well as their antioxidant capacity in human neutrophils has been als...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2007-05, Vol.17 (9), p.2561-2565
Hauptverfasser: Amigó, María, Terencio, María C., Payá, Miguel, Iodice, Carmine, Rosa, Salvatore De
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Sprache:eng
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Zusammenfassung: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-κB activation and TNF-α generation in HaCaT cells as well as their antioxidant capacity in human neutrophils has been also reported. 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-κB activation and TNF-α 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-κB activation with a mild antioxidant pharmacological profile.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.02.007