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

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.

• Authors: Yoann Joyard, Vadim Le Joncour, Hélène Castel, Chérif Bounana Diouf, Laurent Bischoff, Cyril Papamicaël, Vincent Levacher, Pierre Vera, Pierre Bohn
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 23 Issue 13 Pg. 3704-8 (Jul 01 2013) ISSN: 1464-3405 [Electronic] England
• PMID: 23726027 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Published by Elsevier Ltd.

Chemical References

• BRU 59-21
• Imidazoles
• Organotechnetium Compounds

Topics

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