Bis(thiosemicarbazones) as bifunctional chelators for the room temperature 64-copper labeling of peptides

Dalton Trans. 2010 Apr 21;39(15):3620-32. doi: 10.1039/b925128f. Epub 2010 Mar 3.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacokinetics
  • Chelating Agents / chemistry*
  • Coordination Complexes / chemical synthesis
  • Coordination Complexes / chemistry*
  • Coordination Complexes / pharmacokinetics
  • Copper / chemistry*
  • Electron Spin Resonance Spectroscopy
  • Isotope Labeling
  • Ligands
  • Mice
  • Mice, Nude
  • Peptides / chemistry*
  • Temperature
  • Thiosemicarbazones / chemistry*
  • Tissue Distribution
  • Transplantation, Heterologous

Substances

  • Antineoplastic Agents
  • Chelating Agents
  • Coordination Complexes
  • Ligands
  • Peptides
  • Thiosemicarbazones
  • Copper