Synthesis, in vitro binding and biodistribution in B16 melanoma-bearing mice of new iodine-125 spermidine benzamide derivatives.
Nucl Med Biol
; 32(4): 377-84, 2005 May.
Article
in En
| MEDLINE
| ID: mdl-15878507
ABSTRACT
In the course of our investigations aimed at improving the biological characteristics of iodobenzamides for melanoma therapeutic applications, four new derivatives containing a spermidine chain have been prepared and radiolabeled with (125)I. In vitro studies showed that all compounds displayed high affinity for melanin superior to the reference compound BZA, thus validating our experimental approach. In vivo biodistribution was investigated in B16 melanoma-bearing mice. All four compounds, particularly benzamide 3, showed accumulation in the tumor, but lower, however, than that of BZA. Moreover, high concentrations of radioactivity in other organs, namely, the liver and lung, demonstrated nonspecific tumoral uptake. In view of these results, compounds 1 2 3 4 do not appear to be suitable radiopharmaceuticals for melanoma radionuclide therapy.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Benzamides
/
Spermidine
/
Biomarkers, Tumor
/
Iodine Radioisotopes
/
Melanins
/
Melanoma
Limits:
Animals
Language:
En
Journal:
Nucl Med Biol
Journal subject:
BIOLOGIA
/
MEDICINA NUCLEAR
Year:
2005
Type:
Article
Affiliation country:
France