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Radioiodination of 3-amino-2-quinoxalinecarbonitrile 1,4-dioxide and its biological distribution in Erhlich ascites cancer bearing mice as a preclinical tumor imaging agent

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Abstract

3-Amino-2-quinoxalinecarbonitrile 1,4-dioxide (QN) was labeled with 125I, and the biological distribution of the product was studied. 125I-QN was prepared by direct electrophilic substitution reaction using N-bromosuccinimide (NBS) as an oxidizing agent. The radiochemical yield of 92% was reached under the following optimum conditions: pH 7, 15 min, 100 μg of QN, and 75 μg of NBS. The labeled QN was stable for up to 12 h post labeling. Biodistribution study of 125I-QN in tumor-bearing mice reflected that it accumulated in tissues with high proliferation rate with preferential accumulation in tumor sites. 125I-QN was incorporated rapidly in the tumor site (T/NT = 4 at 2 h post injection), and then its content slowly decreased, whereas in the other tissues it decreased rapidly. The results obtained encourage the use of 123I-QN as a tumor imaging agent.

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Authors and Affiliations

  1. Labeled Compounds Department, Hot Laboratories Center, Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt

    I. T. Ibrahim, S. M. Abdelhalim, M. H. Sanad & M. A. Motaleb

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  1. I. T. Ibrahim
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  2. S. M. Abdelhalim
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  3. M. H. Sanad
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  4. M. A. Motaleb
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Correspondence to I. T. Ibrahim.

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Ibrahim, I.T., Abdelhalim, S.M., Sanad, M.H. et al. Radioiodination of 3-amino-2-quinoxalinecarbonitrile 1,4-dioxide and its biological distribution in Erhlich ascites cancer bearing mice as a preclinical tumor imaging agent. Radiochemistry 59, 301–306 (2017). https://doi.org/10.1134/S1066362217030146

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  • DOI: https://doi.org/10.1134/S1066362217030146

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