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Bioorg Med Chem Lett. 2007 Oct 15;17(20):5523-4. Epub 2007 Aug 21.

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

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  • 1UMR 7175 LC1, ULP-CNRS, Faculté de Pharmacie, 67401 Illkirch, France.


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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