2. Academic Validation
  3. Synthesis and evaluation of diverse thio avarol derivatives as potential UVB photoprotective candidates

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

  • Bioorg Med Chem Lett. 2007 May 1;17(9):2561-5. doi: 10.1016/j.bmcl.2007.02.007.
María Amigó 1,  María C Terencio,  Miguel Payá,  Carmine Iodice,  Salvatore De Rosa
Affiliations

Affiliation

  • 1 Departamento de Farmacología, Facultad de Farmacia, Universidad de Valencia, Av. Vicente Andrés Estellés s/n, 46100 Burjasot, Valencia, Spain.
PMID: 17317175 DOI: 10.1016/j.bmcl.2007.02.007
Abstract

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.

Figures