4.5 Article

Synthesis, radioiodination and biological evaluation of a novel phthalimide derivative

Journal

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
Volume 307, Issue 1, Pages 363-372

Publisher

SPRINGER
DOI: 10.1007/s10967-015-4140-3

Keywords

Phthalimide; Pyrazoline; Iodine; Labeling; Tumor

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Biologically active novel phthalimide derivative, N-(5-(2-hydroxyphenyl)-4,5-dihydro-1H-pyrazol-3yl) phthalimide (HPZPHT), was synthesized in excellent yield and characterized by IR, mass and H-1 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). I-131-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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