Synthesis of 3-O-methylviridicatin analogues with improved anti-TNF-alpha properties

  • Bioorg Med Chem Lett. 2007 Oct 15;17(20):5523-4. doi: 10.1016/j.bmcl.2007.08.036.
Nigel Ribeiro  1 ,  Helena Tabaka ,  Jean Peluso ,  Ludivine Fetzer ,  Can Nebigil ,  Serge Dumont ,  Christian D Muller ,  Laurent Désaubry
Affiliations
  • 1. UMR 7175 LC1, ULP-CNRS, Faculté de Pharmacie, 67401 Illkirch, France.
PMID: 17768048 DOI: 10.1016/j.bmcl.2007.08.036
Abstract

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.

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