Synthesis and biological evaluation of a novel (99m)Tc nitrido radiopharmaceutical with deoxyglucose dithiocarbamate, showing tumor uptake

Bioorg Med Chem Lett. 2009 May 15;19(10):2752-4. doi: 10.1016/j.bmcl.2009.03.131. Epub 2009 Mar 28.

Abstract

The deoxyglucose dithiocarbamate (DGDTC) was synthesized and radiolabelled with [(99m)TcN](2+) intermediate to form the (99m)TcN-DGDTC complex. The radiochemical purity of the (99m)TcN-DGDTC complex was over 90%, as measured by TLC and by HPLC, without any notable decomposition at room temperature over a period of 6h. The partition coefficient and electrophoresis results indicated that this complex was hydrophilic and neutral. The biodistribution of (99m)TcN-DGDTC in mice bearing S 180 tumor showed that the complex accumulated in the tumor with high uptake and good retention. The tumor/blood and tumor/muscle ratios increased with time and reached 2.32 and 1.68 at 4h post-injection, suggesting it would be a promising candidate for tumor imaging.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Carbamates / chemical synthesis
  • Carbamates / chemistry
  • Deoxyglucose / analogs & derivatives
  • Deoxyglucose / chemical synthesis
  • Deoxyglucose / chemistry
  • Isotope Labeling
  • Mice
  • Neoplasms / diagnostic imaging*
  • Organotechnetium Compounds / chemical synthesis*
  • Organotechnetium Compounds / chemistry
  • Radionuclide Imaging
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry
  • Tissue Distribution

Substances

  • Carbamates
  • Organotechnetium Compounds
  • Radiopharmaceuticals
  • deoxyglucose dithiocarbamate
  • Deoxyglucose