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Melanoma uptake of (99m)Tc complexes containing the N-(2-diethylaminoethyl)benzamide structural element.

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.
AuthorsMichael Eisenhut, Ashour Mohammed, Walter Mier, Frank Schönsiegel, Matthias Friebe, Ashfaq Mahmood, Alun G Jones, Uwe Haberkorn
JournalJournal of medicinal chemistry (J Med Chem) Vol. 45 Issue 26 Pg. 5802-5 (Dec 19 2002) ISSN: 0022-2623 [Print] United States
PMID12477363 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • 4-(S-benzoyl-2-thioacetyl-glycyl-glycylamido)-N-(2-diethylaminoethyl)benzamide
  • Benzamides
  • Dipeptides
  • Ligands
  • Organotechnetium Compounds
  • Radiopharmaceuticals
Topics
  • Animals
  • Benzamides (chemical synthesis, chemistry, pharmacokinetics)
  • Dipeptides (chemical synthesis, chemistry, pharmacokinetics)
  • Ligands
  • Melanoma (metabolism)
  • Mice
  • Mice, Inbred C57BL
  • Organotechnetium Compounds (chemical synthesis, chemistry, pharmacokinetics)
  • Radiopharmaceuticals (chemical synthesis, chemistry, pharmacokinetics)
  • Tissue Distribution
  • Tumor Cells, Cultured

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