Préparation de prodrogues d'inhibiteurs de kinase : synthèse de phosphoramidates

Abstract : Polycystic kidney disease is the most common genetic disease (PKD1’s mutation or PKD2’s mutation). These mutations create kidney’s cysts. The kidney’s cysts growth increases kidney’s volume; that fact leads to a decreasing in the kidney’s functions and finally a renal failure in 2/3 of the cases. Nowadays, the only treatments consist in kidney dialysis or transplantation which are invasive for patients and expensive for health’s organisms. The thesis’ aim is to develop innovative treatments for this disease. We’ll work on kinase dependant inhibitors (CDKi). Two molecules of this family are showing interesting activities agains polycystic kidney disease. However, because of low bioavailabilities, they can’t be used as treatment. That’s why we tried to synthetise prodrugs in order to evaluate pharmacologic parameters.
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Master Thesis
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Pierre Guery. Préparation de prodrogues d'inhibiteurs de kinase : synthèse de phosphoramidates. Sciences pharmaceutiques. 2019. ⟨dumas-02118503⟩

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