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

Synthesis and biological evaluation of a novel 99mTc labeled 2-nitroimidazole derivative as a potential agent for imaging tumor hypoxia
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DOI:
10.1016/j.bmcl.2013.05.015
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发表时间:
2013-07-01
影响因子:
2.7
通讯作者:
Bohn, Pierre
Bohn, Pierre
中科院分区:
医学4区
文献类型:
--
作者:
Joyard, Yoann;Le Joncour, Vadim;Bohn, Pierre

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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.