Abstract
Various iodo-acridone and acridine carboxamides have been prepared and evaluated as agents for targeted radionuclide and/or chemotherapy for melanoma, due to their structural similarity to benzamides which are known to possess specific affinity for melanin. Three of these carboxamides selected for their in vitro cytotoxic properties were radioiodinated with [(125)I]NaI at high specific activity. Biodistribution studies carried out in B16F0 murine melanoma tumour-bearing mice highlighted that acridone 8f and acridine 9d, presented high, long-lasting tumour concentrations together with an in vivo kinetic profile favourable to application in targeted radionuclide therapy.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acridines / chemical synthesis*
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Acridines / chemistry
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Acridines / pharmacology
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Cell Survival / drug effects
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Cell Survival / radiation effects
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Drug Design
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Humans
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Inhibitory Concentration 50
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Iodine Radioisotopes / administration & dosage*
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Jurkat Cells
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Magnetic Resonance Spectroscopy
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Male
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Melanoma, Experimental / drug therapy*
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Melanoma, Experimental / pathology
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Melanoma, Experimental / radiotherapy*
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Mice
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Mice, Inbred C57BL
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Radionuclide Imaging
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / chemistry
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Radiopharmaceuticals / pharmacology
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Spectrometry, Mass, Electrospray Ionization
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Spectrophotometry, Infrared
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Tissue Distribution
Substances
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Acridines
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Antineoplastic Agents
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Iodine Radioisotopes
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Radiopharmaceuticals