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

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

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Department of Nuclear Medicine, Henri Becquerel Center and Rouen University Hospital and QuantIF-LITIS (EA4108), 1 rue d'Amiens, 76038 Rouen Cedex, France.


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.

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