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

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 radiol...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2013-07, Vol.23 (13), p.3704-3708
Main Authors: Joyard, Yoann, Joncour, Vadim Le, Castel, Hélène, Diouf, Chérif Bounana, Bischoff, Laurent, Papamicaël, Cyril, Levacher, Vincent, Vera, Pierre, Bohn, Pierre
Format: Article
Language:English
Subjects:
2-Nitroimidazole
Biodistribution
Cancer
chemistry
chemotherapy
hypoxia
Hypoxia imaging agent
image analysis
neoplasms
radiolabeling
radiotherapy
rhenium
Scintigraphic image
scintigraphy
Technetium-99m
Tripeptide ligand
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Summary: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 99mTc for imaging hypoxic regions of tumors and was characterized by means of its rhenium analogue. The biodistribution and scintigraphic image of the corresponding 99mTc-complex showed accumulation in tumor and these results suggest that it could be a marker for imaging tumor hypoxia.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2013.05.015