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 |
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Format: | Artikel |
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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2007.02.007 |