Synthesis and biological evaluation of a novel (99m)Tc labeled 2-nitroimidazole derivative as a potential agent for imaging tumor hypoxia

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3704-8. doi: 10.1016/j.bmcl.2013.05.015. Epub 2013 May 16.

Abstract

Tumor hypoxia plays a major role in reducing the efficacy of therapeutic modalities like chemotherapy and radiation therapy in combating cancer. In order to target hypoxic tissues, a tripeptide ligand having a 2-nitroimidazole moiety, as a bioreductive species, was synthesized. The latter was radiolabeled with (99m)Tc for imaging hypoxic regions of tumors and was characterized by means of its rhenium analogue. The biodistribution and scintigraphic image of the corresponding (99m)Tc-complex showed accumulation in tumor and these results suggest that it could be a marker for imaging tumor hypoxia.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Hypoxia*
  • Cell Line, Tumor
  • Glioblastoma* / diagnostic imaging
  • Glioblastoma* / metabolism
  • Glioblastoma* / pathology
  • Humans
  • Imidazoles* / chemistry
  • Imidazoles* / pharmacokinetics
  • Mice
  • Mice, Nude
  • Molecular Structure
  • Organotechnetium Compounds* / chemistry
  • Organotechnetium Compounds* / pharmacokinetics
  • Radionuclide Imaging
  • Tissue Distribution

Substances

  • BRU 59-21
  • Imidazoles
  • Organotechnetium Compounds