title: Design, synthesis and preliminary biological evaluation of acridine compounds as potential agents for a combined targeted chemo-radionuclide therapy approach to melanoma.
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.
authors.affiliation: Univ Clermont 1, UFR Pharmacie, Clermont-Ferrand F-63001, France.
authors.forename: Nicolas
authors.initials: N
authors.lastname: Desbois
authors.forename: Maryline
authors.initials: M
authors.lastname: Gardette
authors.forename: Janine
authors.initials: J
authors.lastname: Papon
authors.forename: Pierre
authors.initials: P
authors.lastname: Labarre
authors.forename: Aurélie
authors.initials: A
authors.lastname: Maisonial
authors.forename: Philippe
authors.initials: P
authors.lastname: Auzeloux
authors.forename: Claire
authors.initials: C
authors.lastname: Lartigue
authors.forename: Bernadette
authors.initials: B
authors.lastname: Bouchon
authors.forename: Eric
authors.initials: E
authors.lastname: Debiton
authors.forename: Yves
authors.initials: Y
authors.lastname: Blache
authors.forename: Olivier
authors.initials: O
authors.lastname: Chavignon
authors.forename: Jean-Claude
authors.initials: JC
authors.lastname: Teulade
authors.forename: Jean
authors.initials: J
authors.lastname: Maublant
authors.forename: Jean-Claude
authors.initials: JC
authors.lastname: Madelmont
authors.forename: Nicole
authors.initials: N
authors.lastname: Moins
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Chezal
mesh_terms: D000166:Acridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects / Q000528:radiation effects; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D007457:Iodine Radioisotopes / Q000008:administration & dosage*; D019169:Jurkat Cells; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008546:Melanoma, Experimental / Q000188:drug therapy* / Q000473:pathology / Q000532:radiotherapy*; D051379:Mice; D008810:Mice, Inbred C57BL; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D021241:Spectrometry, Mass, Electrospray Ionization; D013055:Spectrophotometry, Infrared; D014018:Tissue Distribution
chemical_list: D000166:Acridines; D000970:Antineoplastic Agents; D007457:Iodine Radioisotopes; D019275:Radiopharmaceuticals