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Synthesis and evaluation of a novel 99mTcN(PNP)-complex with metronidazole isocyanide ligand as a marker for tumor hypoxia

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Abstract

The [99mTcN(PNP)]2+ core offers a unique route for the preparation of asymmetric 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 99mTcN(PNP) complex for detecting tumor hypoxia. MetroNC could be prepared in good yield and subsequently radiolabeled with [99mTcN(PNP)]2+ precursor complex prepared from [99mTcN]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.

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Acknowledgments

The authors gratefully acknowledge the support and encouragement provided by Dr. K. L. Ramakmar, Director Radiochemistry & Isotope Group, Bhabha Atomic Research Centre. The authors acknowledge the supply of Molybdenum-99 by Radiochemicals Section, Isotope Production and Application Division. The help rendered by the staff members of the animal house facility of Radiation Biology and Health Sciences Division, is also acknowledged.

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Authors and Affiliations

  1. Radiopharmaceuticals Chemistry Section, Radiochemistry & Isotope Group, Bhabha Atomic Research Centre, Trombay, Mumbai, 400085, India

    Kusum Vats, Madhava B. Mallia & Sharmila Banerjee

  2. Radiation Biology and Health Science Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400085, India

    Haldhar D. Sarma

  3. Medical and Biological Products Program, Board of Radiation and Isotope Technology, Mumbai, 400705, India

    Anupam Mathur

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  1. Kusum Vats
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  2. Madhava B. Mallia
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Correspondence to Sharmila Banerjee.

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Vats, K., Mallia, M.B., Mathur, A. et al. Synthesis and evaluation of a novel 99mTcN(PNP)-complex with metronidazole isocyanide ligand as a marker for tumor hypoxia. J Radioanal Nucl Chem 308, 363–369 (2016). https://doi.org/10.1007/s10967-015-4526-2

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  • DOI: https://doi.org/10.1007/s10967-015-4526-2

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