title: Synthesis, radioiodination and in vivo screening of novel potent iodinated and fluorinated radiotracers as melanoma imaging and therapeutic probes.
abstract: In order to develop new iodinated and fluorinated matched-pair radiotracers for Single-Photon Emission Computed Tomography (SPECT)/Positron Emission Tomography (PET) imaging and targeted radionuclide therapy of melanoma, we successfully synthesized and radiolabelled with iodine-125 seven new derivatives, starting from our previously described lead structure 3. The relevance of these radiotracers for gamma scintigraphic imaging of melanoma in rodent was assessed. The tumoural radioactivity uptake was most often high and specific even at early time points (12.1-18.3% ID/g at 3 h p.i. for [(125)I]39-42) and a fast clearance from the non-target organs was observed. Also, calculated effective doses that could be delivered to tumours when using corresponding [(131)I]-labelled analogues were generally higher than 100 cGy/MBq injected (98.9-150.5 cGy/MBq for [(131)I]39-42). These results make compounds 39-42 suitable candidates for (i) PET imaging of melanoma after labelling with fluorine-18 and (ii) targeted radionuclide therapy of disseminated melanoma after labelling with iodine-131.
authors.affiliation: Clermont Université, Université d'Auvergne, BP 10448, F-63000 Clermont-Ferrand, France. aurelie.maisonial@inserm.fr
authors.forename: Aurélie
authors.initials: A
authors.lastname: Maisonial
authors.forename: Emilie M F
authors.initials: EM
authors.lastname: Billaud
authors.forename: Sophie
authors.initials: S
authors.lastname: Besse
authors.forename: Latifa
authors.initials: L
authors.lastname: Rbah-Vidal
authors.forename: Janine
authors.initials: J
authors.lastname: Papon
authors.forename: Laurent
authors.initials: L
authors.lastname: Audin
authors.forename: Martine
authors.initials: M
authors.lastname: Bayle
authors.forename: Marie-Josèphe
authors.initials: MJ
authors.lastname: Galmier
authors.forename: Sébastien
authors.initials: S
authors.lastname: Tarrit
authors.forename: Michèle
authors.initials: M
authors.lastname: Borel
authors.forename: Serge
authors.initials: S
authors.lastname: Askienazy
authors.forename: Jean-Claude
authors.initials: JC
authors.lastname: Madelmont
authors.forename: Nicole
authors.initials: N
authors.lastname: Moins
authors.forename: Philippe
authors.initials: P
authors.lastname: Auzeloux
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Miot-Noirault
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Chezal
mesh_terms: D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D045744:Cell Line, Tumor; D054879:Halogenation; D007457:Iodine Radioisotopes / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D008297:Male; D008546:Melanoma, Experimental / Q000000981:diagnostic imaging* / Q000628:therapy; D051379:Mice; D008810:Mice, Inbred C57BL; D008956:Models, Chemical; D015394:Molecular Structure; D013997:Time Factors; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon / Q000379:methods*
chemical_list: D001549:Benzamides; D007457:Iodine Radioisotopes; C037689:benzamide