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

Ribeiro, Nigel; Tabaka, Helena; Peluso, Jean; Fetzer, Ludivine; Nebigil, Can; Dumont, Serge; Muller, Christian D; Désaubry, Laurent

Ribeiro, Nigel; Tabaka, Helena; Peluso, Jean; Fetzer, Ludivine; Nebigil, Can; Dumont, Serge; Muller, Christian D; Désaubry, Laurent.

Afiliación

Ribeiro N; UMR 7175 LC1, ULP-CNRS, Faculté de Pharmacie, 67401 Illkirch, France.

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

Article en En | MEDLINE | ID: mdl-17768048

ABSTRACT

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.

Asunto(s)

Hidroxiquinolinas/síntesis química; Hidroxiquinolinas/farmacología; Quinolonas/síntesis química; Quinolonas/farmacología; Factor de Necrosis Tumoral alfa/antagonistas & inhibidores; Factor de Necrosis Tumoral alfa/metabolismo; Células Cultivadas; Humanos; Hidroxiquinolinas/química; Leucocitos/efectos de los fármacos; Leucocitos/metabolismo; Estructura Molecular; Quinolonas/química; Relación Estructura-Actividad

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Bases de datos: MEDLINE Asunto principal: Factor de Necrosis Tumoral alfa / Quinolonas / Hidroxiquinolinas Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2007 Tipo del documento: Article País de afiliación: Francia

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