Bis(thiosemicarbazones) as bifunctional chelators for the room temperature 64-copper labeling of peptides.
A range of new carboxylate functionalised bis(thiosemicarbazone) ligands and their Cu(II) complexes have been prepared, fully characterised and radiolabeled in high yield with both (64)Cu and (99m)Tc. Conjugation to a bombesin derivative was achieved using standard solid phase synthetic methodologies and the (64)Cu-labeled conjugate was shown to have good tumour uptake in mice with xenografted PC-3 tumours.
Hueting
Rebekka
R
Department of Chemistry, Chemistry Research Laboratory, University of Oxford, 12 Mansfield Road, Oxford, OX1 3TA, United Kingdom.
Christlieb
Martin
M
Dilworth
Jonathan R
JR
García Garayoa
Elisa
E
Gouverneur
Véronique
V
Jones
Michael W
MW
Maes
Veronique
V
Schibli
Roger
R
Sun
Xin
X
Tourwé
Dirk A
DA
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D002614:Chelating Agents / Q000737:chemistry*; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D003300:Copper / Q000737:chemistry*; D004578:Electron Spin Resonance Spectroscopy; D007553:Isotope Labeling; D008024:Ligands; D051379:Mice; D008819:Mice, Nude; D010455:Peptides / Q000737:chemistry*; D013696:Temperature; D013882:Thiosemicarbazones / Q000737:chemistry*; D014018:Tissue Distribution; D014183:Transplantation, Heterologous
D000970:Antineoplastic Agents; D002614:Chelating Agents; D056831:Coordination Complexes; D008024:Ligands; D010455:Peptides; D013882:Thiosemicarbazones; D003300:Copper