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Synthèse et évaluation biologique de nouveaux composés hétérocycliques potentiellement inhibiteurs de protéine-kinases

Abstract : Deregulation of protein kinases leads to numerous pathologies such as cancers and neurodegenerative diseases. In order to identify new scaffolds able to inhibit this proteins we synthesized new 3-alkenyl-oxindoles. By the mean of Appel’s salt chemistry, we develop a new synthetic route to this skeleton. Our approach allows variation of the substituent of the exocyclic akene which can be functionalized by heterocycles, amino-nitriles or thio-nitrile which are obtained after selective ring opening of (1,2,3)-dithiazoles. In another part, given powerful indirubin kinase inhibitory potency, we synthesized new analogs indiribunoids and isoindigoids. In both cases (3-akenyl-oxindoles from Appel’s salt chemistry and indigoids), the aromatic ring were substituted by various electron withdrawing group and nitrogen were incorporated to determinate structure activity relationship. All this 80 original 3-alkenyl-oxindoles were evaluated for their ability to inhibit kinase activity and cell proliferation.
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https://tel.archives-ouvertes.fr/tel-01694272
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Boris Letribot. Synthèse et évaluation biologique de nouveaux composés hétérocycliques potentiellement inhibiteurs de protéine-kinases. Chimie organique. Université de La Rochelle, 2015. Français. ⟨NNT : 2015LAROS002⟩. ⟨tel-01694272⟩

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