Synthesis and evaluation of a novel .sup.99mTcN-complex with metronidazole isocyanide ligand as a marker for tumor hypoxia

The [.sup.99mTcN(PNP)].sup.2+ core offers a unique route for the preparation of asymmetric .sup.99mTc-complexes. Though bidentate chelators such as dithiocarbamates are most commonly used ligands in this approach, present study explores the possibility of using a monodentate ligand, a isocyanide der...

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Published in:Journal of radioanalytical and nuclear chemistry 2016-04, Vol.308 (1), p.363
Main Authors: Vats, Kusum, Mallia, Madhava B, Mathur, Anupam, Sarma, Haldhar D, Banerjee, Sharmila
Format: Article
Language:English
Subjects:
Antiprotozoan agents
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Summary:The [.sup.99mTcN(PNP)].sup.2+ core offers a unique route for the preparation of asymmetric .sup.99mTc-complexes. Though bidentate chelators such as dithiocarbamates are most commonly used ligands in this approach, present study explores the possibility of using a monodentate ligand, a isocyanide derivative of metronidazole (MetroNC), for preparing a .sup.99mTcN(PNP) complex for detecting tumor hypoxia. MetroNC could be prepared in good yield and subsequently radiolabeled with [.sup.99mTcN(PNP)].sup.2+ precursor complex prepared from [.sup.99mTcN].sup.2+ core and N-(2-methoxyethyl)-2-(diphenylphosphino)-N-(2-(diphenylphosphino)ethyl)ethanamine (PNP2) ligand. Preliminary biodistribution studies showed tumor uptake pattern similar to previous studies wherein, about 75 % of the tumor activity observed at 60 min post injection (p.i.) was still found to remain in tumor at 180 min p.i.
ISSN:0236-5731
DOI:10.1007/s10967-015-4526-2