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Complexes of 1,4,7-triazacyclononane phosphinate derivatives
Lebruška, Viktor ; Kubíček, Vojtěch (advisor) ; Štěpnička, Petr (referee)
Phosphorus pendant arms accelerate the complexation of gallium(III) ions with macrocyclic chelators, which is crucial parameter in labelling by the radioisotope 68 Ga and their use in positron emission tomography (PET). In this thesis, new chelators for the selective complexation of gallium(III) ions were designed. Two chelators derived from the TACN macrocycle were prepared, namely: 1,4,7-triazacyclononane-1-methyl-methylene- bis(phosphinic) acid (H2L1 ) and 1,4,7-triazacyclononane-1-methyl-methylene- bis(phosphinato)-4,7-bis(methyl-phosphinic) (H4L2 ). The acidobase properties of the H2L1 were investigated using potentiometric and NMR titrations. Complexes of H2L1 with Ni(II), Cu(II), Zn(II) and Ga(III) were investigated using potentiometric titrations, which showed the high stability of these complexes. The solid-state structures of the Cu-L1 and Zn-L1 complexes were determined by X-ray diffraction. Complexation of the radioisotope 68 Ga(III) was studied for chelators H2L1 , H4L2 and for several related chelators with phosphorus pendant arms. The complexation study showed that chelators with the methylene-bis(phosphinate) pendant arm and some other phosphorus chelators derived from the TACN macrocycle accelerate complexation of gallium(III) ions. Using Dynamic PET scanning and ex-vivo...
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Complexes of 1,4,7-triazacyclonane for nuclear medicine
Lebruška, Viktor ; Kubíček, Vojtěch (advisor) ; Schulz, Jiří (referee)
The use of metal isotopes for the study of tissues in the field of nuclear medicine is currently being developed. Metal isotopes are accumulated non-specifically in the body. Therefore, it is necessary for diagnosis and therapy to use suitable ligands, which form a thermodynamically stable and kinetically inert complex with the given metal ion, which can be attached to a suitable targeting group. Isotopes of gallium and copper are suitable for imaging od therapy. The cavity of the 1,4,7-triazacyclononane is suitable for the complexation of gallium, copper and some other metals with a small radius. However, the macrocycle itself does not form thermodynamically stable complexes, so the nitrogen atoms must be substituted by proper pendant arms, such as carboxylates. In recent years organic residues of phosphoric acids are also used. This work deals with substances that are derivatives of 1,4,7-triazacyclononane and contain phosphorus arms, which were studied in recent years. Keywords complexes, ligands, dissociation constants, stability constants
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