Synthesis and in vitro/vivo Evaluation of Iodine-123/124 Labelled Hypericin Derivatives

doi:10.5012/bkcs.2008.29.10.2023

Bulletin of the Korean Chemical Society

2008

DOI: 10.5012/bkcs.2008.29.10.2023

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Synthesis and in vitro/vivo Evaluation of Iodine-123/124 Labelled Hypericin Derivatives

Abstract: To evaluate the potential of radioiodine labelled hypericin as a malignant glioma imaging agent, U-251 MG, U-373 MG, C6 glioma and fibroblast were treated with a I-123 labelled hypericin derivative and C6 glioma transplanted nude mouse were injected with a I-124 labelled hypericin derivative for a micro PET imaging. 2-Iodohypericin was prepared as a reference compound. In this paper, we describe the syntheses of 2-iodohypericin and 2-[

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Cited by 6 publications

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Design of Radioiodinated Pharmaceuticals: Structural Features Affecting Metabolic Stability towards in Vivo Deiodination

Cavina

Born²,

Klaren

et al. 2017

Eur J Org Chem

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Radioiodinated pharmaceuticals are convenient tracers for clinical and research investigations because of the relatively long half‐lives of radioactive iodine isotopes (i.e., 123I, 124I, and 131I) and the ease of their chemical insertion. Their application in radionuclide imaging and therapy may, however, be hampered by poor in vivo stability of the C–I bond. After an overview of the use of iodine in biology and nuclear medicine, we present here a survey of the catabolic pathways for iodinated xenobiotics, including their biodistribution, accumulation, and biostability. We summarize successful rational improvements in the biostability and conclude with general guidelines for the design of stable radioiodinated pharmaceuticals. It appears to be necessary to consider the whole molecule, rather than the radioiodinated fragment alone. Iodine radionuclides are generally retained in vivo on sp2 carbon atoms in iodoarenes and iodovinyl moieties, but not in iodinated heterocycles or on sp3 carbon atoms. Iodoarene substituents also have an influence, with increased in vivo deiodination in the cases of iodophenols and iodoanilines, whereas methoxylation and difluorination improve biostability.

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Design of Radioiodinated Pharmaceuticals: Structural Features Affecting Metabolic Stability towards in Vivo Deiodination

Cavina

Born²,

Klaren

et al. 2017

Eur J Org Chem

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Current Awareness in Labelled Compounds and Radiopharmaceuticals

2009

Labelled Comp Radiopharmac

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In order to keep subscribers up‐to‐date with the latest developments in their field, John Wiley & Sons are providing a current awareness service in each issue of the journal. The bibliography contains newly published material in the field of labelled compounds and radiopharmaceuticals. Each bibliography is divided into 16 sections: 1 Radionuclide Production; 2 Labelled Compound Synthesis; Applications: 3 Biomedical ‐ General; 4 Imaging ‐ General; 5 Fluorine; 6 Carbon; 7 Technetium; 8 Iodine; 9 Copper; 10 Gallium; 11 Indium; 12 Hydrogen; 13 Others; 14 Therapy; 15 Environmental; 16 Analytical Techniques. Within each section, articles are listed in alphabetical order with respect to author. If, in the preceding period, no publications are located relevant to any one of these headings, that section will be omitted.

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Critical analysis of radioiodination techniques for micro and macro organic molecules

Mushtaq

Jeon

Shaheen

et al. 2016

J Radioanal Nucl Chem

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Synthesis and in vitro/vivo Evaluation of Iodine-123/124 Labelled Hypericin Derivatives

Cited by 6 publications

References 16 publications

Design of Radioiodinated Pharmaceuticals: Structural Features Affecting Metabolic Stability towards in Vivo Deiodination

Design of Radioiodinated Pharmaceuticals: Structural Features Affecting Metabolic Stability towards in Vivo Deiodination

Current Awareness in Labelled Compounds and Radiopharmaceuticals

Critical analysis of radioiodination techniques for micro and macro organic molecules

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