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

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.

• Authors: Junbo Zhang, Jialei Ren, Xiao Lin, Xuebin Wang
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 19 Issue 10 Pg. 2752-4 (May 15 2009) ISSN: 1464-3405 [Electronic] England
• PMID: 19362469 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

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

Topics

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