By Krause W.
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47 Abstract This review presents a comprehensive overview of the most significant developments in the chemistry of technetium and rhenium complexes anchored by heterofunctionalized phosphines and by hard and soft scorpionates. The main goal is to provide the reader with chemical, radiochemical and biological knowledge which is expected to enhance the application of these types of compounds in the development of target-specific radiopharmaceuticals.
However, as a folate-receptortargeted radiopharmaceutical, the radiotracer does not appear to offer advantages over other folate–chelate conjugates . Whereas the synthesis of compounds which are antagonists for hexokinase could probably be achieved (the 3D structure of hexokinase is known), it is much more difficult to transport such radiopharmaceuticals through the glucose transporter of the cell membrane. In a recent study, an imino-diacetate based chelator was introduced at C1. Labelling with fac-[99mTc(CO)3]+ gave one product but the glucose conjugate did not show any uptake in cells .
The acetyl group can act as an anchoring group for biomolecules. The general strategy of reacting NaCp with an ester results in the formation of a Cp–CO–biomolecule conjugate. This approach has been described with the serotonergic receptor ligands WAY, one of the most thoroughly investigated CNS receptor ligand. Some of the compounds are shown in Scheme 20. Reaction with [99Tc(OH2)3(CO)3]+ in phosphate buffer gave the corresponding 99Tc complexes. The X-ray structure of a model complex is shown in Fig.
Contrast Agents III by Krause W.