Melanoma uptake of (99m)Tc complexes containing the N-(2-diethylaminoethyl)benzamide structural element.
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.
Eisenhut
Michael
M
German Cancer Research Center, University of Heidelberg, Heidelberg, Germany. m.eisenhut@dkfz.de
Mohammed
Ashour
A
Mier
Walter
W
Schönsiegel
Frank
F
Friebe
Matthias
M
Mahmood
Ashfaq
A
Jones
Alun G
AG
Haberkorn
Uwe
U
D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D004151:Dipeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D008024:Ligands; D008545:Melanoma / Q000378:metabolism*; D051379:Mice; D008810:Mice, Inbred C57BL; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D014018:Tissue Distribution; D014407:Tumor Cells, Cultured
C470211:4-(S-benzoyl-2-thioacetyl-glycyl-glycylamido)-N-(2-diethylaminoethyl)benzamide; D001549:Benzamides; D004151:Dipeptides; D008024:Ligands; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals