5 years ago

Gallium Complexation, Stability, and Bioconjugation of 1,4,7-Triazacyclononane Derived Chelators with Azaheterocyclic Arms

Gallium Complexation, Stability, and Bioconjugation of 1,4,7-Triazacyclononane Derived Chelators with Azaheterocyclic Arms
Mark D. Bartholomä, Manfred Keller, Alexander Schmidtke, Lorenz Bier-Schorr, Tilman Läppchen, Jason P. Holland, Christian Weinmann, Yvonne Kiefer
We recently demonstrated the applicability of 1,4,7-triazacyclononane derived ligands with up to three azaheterocyclic arms as chelating agents for 64Cu used in positron emission tomography (PET). Here, we describe their complex formation with the PET isotope 68Ga3+. These ligands form rigid 1:1 chelates with natGa3+ in solution. In 68Ga3+ complexes of the five-coordinate bifunctional chelator NODIA-Me, the remaining coordination site of the octahedron is occupied by monodentate ligands such as chloride or hydroxide.

Publisher URL: http://dx.doi.org/10.1021/acs.inorgchem.7b01129

DOI: 10.1021/acs.inorgchem.7b01129

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