Abstract
On the basis of the avid uptake of radioiodinated benzamides by melanoma cells, (99m)Tc complexes containing the structural elements of N-(dialkylaminoalkyl)benzamide pharmacophores have been synthesized and evaluated in vitro and in vivo for melanoma uptake. One of the complexes Tc-12 containing the ligand 4-(S-benzoyl-2-thioacetyl-glycyl-glycylamido)-N-(2-diethylaminoethyl)benzamide (11) displayed the highest melanoma uptake. The 1-h melanoma uptake values and the corresponding blood counts indicate an interdependence of tumor uptake and bioavailability of the (99m)Tc complexes.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Benzamides / chemical synthesis*
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Benzamides / chemistry
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Benzamides / pharmacokinetics
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Dipeptides / chemical synthesis*
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Dipeptides / chemistry
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Dipeptides / pharmacokinetics
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Ligands
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Melanoma / metabolism*
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Mice
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Mice, Inbred C57BL
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Organotechnetium Compounds / chemical synthesis*
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Organotechnetium Compounds / chemistry
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Organotechnetium Compounds / pharmacokinetics
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / chemistry
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Radiopharmaceuticals / pharmacokinetics
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Tissue Distribution
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Tumor Cells, Cultured
Substances
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4-(S-benzoyl-2-thioacetyl-glycyl-glycylamido)-N-(2-diethylaminoethyl)benzamide
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Benzamides
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Dipeptides
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Ligands
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Organotechnetium Compounds
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Radiopharmaceuticals