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Synthèse de composés possédant un motif de type oxindole, inhibiteurs potentiels du récepteur de facteur de croissance de fibroblastes (FGFR1)

Abstract : The growth factors receptors are overexpressed in a great number of cancers and play a very important role in cell proliferation. We were interested in the ATP competitive inhibitors of the tyrosine kinase domain of the growth factors receptors, more particularly of the FGFR1. This receptor constitutes a privileged target for the development of new anti-cancer agents. The first part of this work is a bibliographical study on growth factors receptors. The principal families of growth factors receptors inhibitors are detailed. To design a new model of inhibitors of the FGFR1 tyrosine kinase activity, we prepared three families of compounds. The synthesis of these compounds is reported in the second part. The third part, presents a study of docking and energy minimization by molecular mechanics on the complexes of some of the synthesized compounds in the FGFR1 ATP-site. In the fourth part, the cytoxicity on various tumor and healthy cell lines and the inhibitory activity on various kinases of the new products prepared during this work are detailed.
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  • HAL Id : tel-00683658, version 1

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Mathieu Sassatelli. Synthèse de composés possédant un motif de type oxindole, inhibiteurs potentiels du récepteur de facteur de croissance de fibroblastes (FGFR1). Chimie organique. Université Blaise Pascal - Clermont-Ferrand II, 2005. Français. ⟨NNT : 2005CLF21609⟩. ⟨tel-00683658⟩

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