Abstract
Technetium-99m has a rich coordination chemistry that offers many possibilities in terms of oxidation states and donor atom sets. Modifications in the structure of the technetium complexes could be very useful for fine tuning the physicochemical and biological properties of potential 99mTc radiopharmaceuticals. However, systematic study of the influence of the labelling strategy on the “in vitro” and “in vivo” behaviour is necessary for a rational design of radiopharmaceuticals. Herein we present a review of the influence of the Tc complexes’ molecular structure on the biodistribution and the interaction with the biological target of potential nitroimidazolic hypoxia imaging radiopharmaceuticals presented in the literature from 2010 to the present. Comparison with the gold standard [18F]Fluoromisonidazole (FMISO) is also presented.
Highlights
Technetium-99m has a rich coordination chemistry that offers many possibilities in terms of oxidation states and donor atom sets
Introduction of technetium is associated with a change in the spatial configuration of the bioactive molecule which can significantly affect the interaction with the target
In order to contribute to the rational design of potential [99m Tc]Tc radiopharmaceuticals we proposed to review the influence of the Tc complexes molecular structure on the biodistribution and the interaction with the biological target of potential hypoxia imaging radiopharmaceuticals presented in the literature from 2010 to 2019
Summary
The design of potential 99m Tc radiopharmaceuticals for molecular imaging is currently based almost exclusively on the application of the so-called “bifunctional approach” consisting of the combination of a biologically active molecule with a chelating unit for stable binding of the radiometal. Both parts are separated by a linker chain to avoid interference of the metal complex in the interaction with the target. Inorganics 2019, 7, 128 agents were chosen because of the considerable interest in the subject demonstrated by the extensive literature available and because in spite of the research performed so far no agent with adequate properties has been proposed
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