Bioconjugated technetium carbonyls by transmetalation reaction with zinc derivatives

Bioorg Med Chem Lett. 2021 Apr 1:37:127840. doi: 10.1016/j.bmcl.2021.127840. Epub 2021 Feb 5.

Abstract

The transmetalation reaction between zinc dithiocarbamates functionalized with organic groups and the cation fac-[99mTc(H2O)3(CO)3]+ has been studied as a new strategy to bind biomolecules to this radionuclide for preparing radiopharmaceuticals with high molar activity. All complexes were obtained in high yields by heating at moderate temperatures and without subsequent purification. The chemical identity was ascertained by HPLC comparison with the homologous rhenium complexes. Stability studies in cysteine solution and serum have shown a good stability of the coordination set fac-[99mTc(CO)3(SS)(P)]. Preliminary biological studies of the radiocomplex functionalized with D-(+)-glucosamine with carcinoma cells have been performed.

Keywords: Carbonyl; Radiopharmaceutical; Rhenium; Technetium; Transmetallation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Coordination Complexes / administration & dosage
  • Coordination Complexes / chemistry*
  • Coordination Complexes / pharmacokinetics
  • Mice
  • Radiopharmaceuticals / administration & dosage
  • Radiopharmaceuticals / chemistry*
  • Radiopharmaceuticals / pharmacokinetics
  • Single Photon Emission Computed Tomography Computed Tomography
  • Technetium / administration & dosage
  • Technetium / chemistry
  • Technetium / pharmacokinetics*
  • Tissue Distribution
  • Zinc / administration & dosage
  • Zinc / chemistry*
  • Zinc / pharmacokinetics

Substances

  • Coordination Complexes
  • Radiopharmaceuticals
  • Technetium
  • Zinc