Synthesis of 3-O-methylviridicatin analogues with improved anti-TNF-alpha properties.
Fiche publication
Date publication
octobre 2007
Auteurs
Membres identifiés du Cancéropôle Est :
Dr DESAUBRY Laurent, Dr NEBIGIL-DESAUBRY Canan
Tous les auteurs :
Ribeiro N, Tabaka H, Peluso J, Fetzer L, Nebigil C, Dumont S, Muller CD, Desaubry L
Lien Pubmed
Résumé
We synthesized 3-O-methylviridicatin and several analogues of this fungal metabolite. We showed that replacement of the methoxy moiety by a thiomethyl enhanced dramatically its ability to inhibit TNF-alpha secretion. These results strongly suggest that 4-phenyl-3-methylthioquinolinone may provide the basis for the development of new anti-inflammatory agents.
Référence
Bioorg Med Chem Lett. 2007 Oct 15;17(20):5523-4