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Synthesis, radioiodination and biological evaluation of a novel phthalimide derivative

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Abstract

Biologically active novel phthalimide derivative, N-(5-(2-hydroxyphenyl)-4,5-dihydro-1H-pyrazol-3-yl)phthalimide (HPZPHT), was synthesized in excellent yield and characterized by IR, mass and 1H NMR spectroscopy. It was radiolabeled with iodine-131 by direct electrophilic substitution reaction and radiochemical yield was determined by using different chromatographic techniques (HPLRC, paper chromatography and paper electrophoresis). 131I-HPZPHT has high radiolabeling yield (98.00 ± 2.00 %), stability, solid tumor uptake and T/NT ratio (5.17 ± 0.03 at 30 min. post-injection) compared with many new tracers which have been developed in recent years. This study encourages the possible use of this tracer as a potential imaging and/or therapeutic agent for cancer.

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Authors and Affiliations

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

    M. A. Motaleb, I. Y. Abdel-Ghaney & H. A. Shamsel-Din

  2. Faculty of Science, Menoufia University, Cairo, Egypt

    H. M. Abdel-Bary

Authors
  1. M. A. Motaleb
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  2. I. Y. Abdel-Ghaney
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  3. H. M. Abdel-Bary
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  4. H. A. Shamsel-Din
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Correspondence to H. A. Shamsel-Din.

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Motaleb, M.A., Abdel-Ghaney, I.Y., Abdel-Bary, H.M. et al. Synthesis, radioiodination and biological evaluation of a novel phthalimide derivative. J Radioanal Nucl Chem 307, 363–372 (2016). https://doi.org/10.1007/s10967-015-4140-3

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  • DOI: https://doi.org/10.1007/s10967-015-4140-3

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