Conception, Synthèse et Évaluation Biologique d'Hétéroarylimino-1,3-thiazolidin-4-ones à Activité anti-cancéreuse potentielle

Abstract : Cancer, which is the first cause of death care in developed countries, is a disease from various origins, and characterized by an uncontrolled proliferation of abnormal cells. This proliferation is mainly caused by a deregulation of the cell cycle, which usually provides the renewal of the organism cells. Many treatments are currently used to fight this disease, but showing important adverse effects. For this reason, the development of new antitumor compounds appears as a major challenge in medicinal chemistry. Among the investigated compounds, thiazolidinone derivatives appear as particularly interesting, especially due to the variety of targets they are described to interact with. Thus, we performed the design, synthesis and biological evaluation of new series of variously functionalized 2-iminothiazolidinones, starting from heterocycles already investigated in the laboratory (thiophene, selenophene, thiazole), but also from new precursors developed during our investigations. Determination of the antiproliferative activity of those compounds allowed to isolate some promising structures, showing IC50 values in micromolar range on investigated cell lines, maybe due to the inhibition of CDC25 phosphatases, which are responsible of the cell cycle regulation
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Germain Revelant. Conception, Synthèse et Évaluation Biologique d'Hétéroarylimino-1,3-thiazolidin-4-ones à Activité anti-cancéreuse potentielle. Autre. Université de Lorraine, 2012. Français. ⟨NNT : 2012LORR0078⟩. ⟨tel-01749292⟩

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