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Synthèse d'antagonistes osidiques du récepteur de la vitronectine

Abstract : In the present works at the interface chemistry-biology, we took an interest in the cellular and molecular adhesion processes responsible for many pathological disorders. We focused particularly on the RGD-relevant binding of many natural ligands to a specific receptor, the alpha v beta 3 integrin. Therefore, we realised carbohydrate-based peptidomimetics of this key tripeptide as potential therapeutic agents for the treatment of chronic inflammation or cancerous tumours. In the first part of this study, we applied the parallel chemistry methods to a carbohydrate template and thus, we prepared a first library of antagonists. In order to improve the potency of our compounds, we used molecular modelling to obtain a three-dimensional model of the pharmacophore. With the new geometrical data obtained, two bicyclic sugar amino acid hybrids were designed. These structures should allow a spatial refinement of the essential groups responsible for the activity. To validate our approach, we finally achieved the gram-scaled synthesis for both of these chiral scaffolds.
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Submitted on : Thursday, March 29, 2018 - 10:42:44 AM
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  • HAL Id : tel-01746688, version 1



Christophe Henry. Synthèse d'antagonistes osidiques du récepteur de la vitronectine. Autre. Université Henri Poincaré - Nancy 1, 2001. Français. ⟨NNT : 2001NAN10265⟩. ⟨tel-01746688⟩



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