Preparation and biodistribution of a (99m)Tc tricarbonyl complex with deoxyglucose dithiocarbamate as a tumor imaging agent for SPECT

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3964-7. doi: 10.1016/j.bmcl.2014.06.037. Epub 2014 Jun 21.

Abstract

The deoxyglucose dithiocarbamate (DGDTC) was successfully labeled with the (99m)Tc(CO)3 core to provide the corresponding (99m)Tc(CO)3-DGDTC complex in good yields. The radiochemical purity of the (99m)Tc(CO)3-DGDTC complex was over 90%, as measured by high performance liquid chromatography (HPLC). The complex possessed good stability in saline at room temperature and in mouse plasma at 37 °C. Its partition coefficient result indicated that it was a hydrophilic complex. The electrophoresis results showed the complex was neutral. The biodistribution of (99m)Tc(CO)3-DGDTC in mice bearing S 180 tumor showed that the complex clearly accumulated in tumor, exhibiting high tumor/blood and tumor/muscle ratios and good tumor retention. Single photon emission computed tomography (SPECT) image studies showed there was a visible uptake in tumor sites, suggesting (99m)Tc(CO)3-DGDTC could be considered as a potential tumor imaging agent.

Keywords: (99m)Tc tricarbonyl complex; Deoxyglucose; Dithiocarbamate; Tumor imaging agent.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Carbamates / chemistry*
  • Deoxyglucose / analogs & derivatives*
  • Deoxyglucose / chemistry
  • Mice
  • Organotechnetium Compounds / chemistry
  • Organotechnetium Compounds / pharmacokinetics*
  • Sarcoma 180 / drug therapy*
  • Tissue Distribution
  • Tomography, Emission-Computed, Single-Photon*

Substances

  • Carbamates
  • Organotechnetium Compounds
  • deoxyglucose dithiocarbamate
  • Deoxyglucose