Synthèse et coordination de triazacyclononanes et de dérivés bifonctionnels : vers des applications en imageries médicales

Abstract : The 1,4,7-triazacyclononane (tacn) is part of the family of polyazamacrocycles, and has the faculty, when appropriately N-functionalized with coordination pendants, to form thermodynamically stable and kinetically inert coordination complexes with transition metals. Thanks to their properties tacn derivatives can be found in numerous applications such as medical imaging. Our group has developed some ligands N-functionalized with picolinate and picolyl pendants for an application in PET imaging and MRI.The first part of this thesis is focused on the development of a new class of bimodal PET-optical imaging and MRI-optical imaging probes based on tacn-picolinate units described in the laboratory.The second part deals with the synthesis of new Cu(II) chelators based on tacn-methylthiazolyl units for a potential application in PET imaging. The corresponding Cu(II) complexes were studied by different analytical and spectroscopic methods in order to evaluate their thermodynamic stabilities and kinetic inertness.The chelators that fullfiled all the criterias imposed by the biological media were selected for an applicationPET imaging of prostate cancer. Some bifunctional analogues were elaborated so as to incorporate them in radiopharmaceuticals radiolabeled with copper-64.
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Amaury Guillou. Synthèse et coordination de triazacyclononanes et de dérivés bifonctionnels : vers des applications en imageries médicales. Chimie. Université de Bretagne occidentale - Brest, 2018. Français. ⟨NNT : 2018BRES0081⟩. ⟨tel-02110360⟩

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