Synthesis and biological evaluation of a novel Tc-99m 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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Published inBioorganic & medicinal chemistry letters Vol. 23; no. 13; pp. 3704 - 3708
Main Authors Joyard, Yoann, Le Joncour, Vadim, Castel, Helene, Diouf, Cherif Bounana, Bischoff, Laurent, Papamicael, Cyril, Levacher, Vincent, Vera, Pierre, Bohn, Pierre
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier 01.07.2013
Subjects
Chemistry
Chemistry, Medicinal
Chemistry, Organic
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Physical Sciences
Science & Technology
Scintigraphic image
NITROIMIDAZOLES
Hypoxia imaging agent
IN-VITRO EVALUATION
MARKER
2-Nitroimidazole
COMPLEXES
Tripeptide ligand
Biodistribution
Technetium-99m
BISNITROIMIDAZOLE
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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 Tc-99m for imaging hypoxic regions of tumors and was characterized by means of its rhenium analogue. The biodistribution and scintigraphic image of the corresponding Tc-99m-complex showed accumulation in tumor and these results suggest that it could be a marker for imaging tumor hypoxia. Published by Elsevier Ltd.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2013.05.015