A new hexaazamacrobicyclic cage ligand, 1-N-(4-aminobenzyl)- 3,6,10,13,16,19-hexaazabicyclo[6.6.6]eicosane-1,8-diamine (SarAr) has been designed for conjugation to proteins. SarAr was synthesised and characterised by microanalyses, 1 H NMR and electrospray mass spectrometry. The complexation of selected transition metal ions (Cu(), Ni() and Co() at 10 Ϫ6 M) by SarAr was complete within 30 min over pH 6 to 8. The [ 64 Cu(SarAr)] 2ϩ complex was investigated with a view to applications in radioimaging. The [ 64 Cu(sar)] 2ϩ complex was found to be stable in human plasma for at least 174 h and biodistribution studies in mice, showed that the [ 64 Cu(SarAr)] 2ϩ complex was rapidly excreted through the renal system unlike the free 64 Cu 2ϩ . Overall, the simple synthesis, ready complexation behaviour of SarAr, the kinetic inertness of the [Cu(SarAr)] 2ϩ complex to dissociation of 64 Cu and its facile elimination from mice make it an attractive prospect for use in nuclear medicine.
The synthesis of macrocyclic ligands that contain appended side chains incorporating potentially reactive donor functions has been of recent interest. The bifunctional nature of these ligands, with one site possessing a high affinity for the metal ion and a second site with a chemically reactive group suitable for further elaboration, has found many applications in the attachment of the ligands to polymers and biomolecules.2'18 There are, however,
The binuclear octahedral MI1 complexes, incorporating the new 10 coordinate pendant arm ligand LH4,t all show an anti-configuration; in contrast the Cull complex [Cu,(LH2)]2+ adopts a syn-configuration incorporating intramolecular H-bonding.
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