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, Synthèse des aldéhydes de la chromone par réaction Vilsmeier-Haack: exemple 50, vol.9

, Les produits de départ 50-58 ont été préparés par la réaction de Vilsmeier-Haack, vol.21, pp.70-80

, Cette méthode peut être utilisée pour formyler des systèmes aromatiques activés dans le sens d'une acylation de Friedl-Crafts à cause de l'instabilité du dérivé chloroformylé [81]. Les benzofuranones 59a,b et 60 ont été préparées selon une méthode développée dans notre laboratoire, vol.82, p.61

, Voie de synthèse a: Al 2 O 3 (acide), DCM anhydre, température ambiante, Schéma, vol.11, pp.2-6

. Enfin, nous avons réalisé la condensation aldolique de l'aldéhyde avec le benzofurane par l'utilisation de l'Al 2 O 3 acétique (Brockmann I), vol.26, pp.61-70

, particulièrement celles, qui concernent les activités anti-inflammatoires et anticancéreuses, vol.211

, Les chalcones, naturelles et synthétiques, comme 106, sont rapportées dans la bibliographie comme inhibiteurs de la voie de signalisation NF-kB

, Des études in vitro ont montré qu'il y a un effet cytotoxique par plusieurs voies, comme NF-kB, MAPK, STAT3 ou voie Wnt, vol.227, pp.242-244

. Appendino, ont extrait un sesquiterpene coumarinique 109 d'Asafetida comme un fort inhibiteur spécifique de NF-kB [258]. Par conséquence, les coumarines pourraient être intéressantes comme un motif structural différent

, Nous avons combiné ces motifs structuraux pour créer une nouvelle série de chalcones avec une base coumarinique. Les composés 112a-g, portant un cétone ?, ?-mono-insaturé à la position C3, sont préparés par une condensation aldolique entre la 3-acétylcoumarine, précédemment synthétisée par notre laboratoire selon la bibliographie, Synthèse des dérivés coumariniques 112a-g, vol.18

, Tout d'abord, nous avons étudié l'aptitude potentielle de toutes nouvelles molécules pour moduler la voie NF-?B, induite par le TNF?. Jusqu'à présent nous nous n'avons pas réussi à montrer l'implication de nos composés à la voie NF-?B

, Par conséquence, aucun résultat biologique ne peut être présenté jusqu'à présent

, Des études complémentaires et plus approfondies doivent être menées afin d'estimer les propriétés biologiques de ces composés dans la participation éventuelle aux voies différentes. Dans l'avenir, nous devrons valider la cible biologique parallèlement à l'optimisation de notre stratégie de conception et de

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