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Melanoma-targeted delivery system (part 2): Synthesis, radioiodination and biological evaluation in B16F0 bearing mice.
El Aissi, Radhia; Miladi, Imen; Chezal, Jean-Michel; Chavignon, Olivier; Miot-Noirault, Elisabeth; Moreau, Emmanuel.
Affiliation
  • El Aissi R; INSERM - Université d'Auvergne, UMR 990, IMTV, BP 184, F-63005 Clermont-Ferrand Cedex, France; Clermont Université, Université d'Auvergne, Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63005 Clermont-Ferrand Cedex, France.
  • Miladi I; INSERM - Université d'Auvergne, UMR 990, IMTV, BP 184, F-63005 Clermont-Ferrand Cedex, France; Clermont Université, Université d'Auvergne, Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63005 Clermont-Ferrand Cedex, France.
  • Chezal JM; INSERM - Université d'Auvergne, UMR 990, IMTV, BP 184, F-63005 Clermont-Ferrand Cedex, France; Clermont Université, Université d'Auvergne, Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63005 Clermont-Ferrand Cedex, France.
  • Chavignon O; INSERM - Université d'Auvergne, UMR 990, IMTV, BP 184, F-63005 Clermont-Ferrand Cedex, France; Clermont Université, Université d'Auvergne, Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63005 Clermont-Ferrand Cedex, France.
  • Miot-Noirault E; INSERM - Université d'Auvergne, UMR 990, IMTV, BP 184, F-63005 Clermont-Ferrand Cedex, France; Clermont Université, Université d'Auvergne, Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63005 Clermont-Ferrand Cedex, France.
  • Moreau E; INSERM - Université d'Auvergne, UMR 990, IMTV, BP 184, F-63005 Clermont-Ferrand Cedex, France; Clermont Université, Université d'Auvergne, Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63005 Clermont-Ferrand Cedex, France. Electronic address: emmanuel.moreau@udamail.fr.
Eur J Med Chem ; 120: 304-12, 2016 Sep 14.
Article in En | MEDLINE | ID: mdl-27214141
ABSTRACT
Here we report the synthesis and radiolabelling with iodine-125 of a melanoma-selective prodrug (17a*) and its parent drug IUdR. The in vivo and ex vivo biodistributions of [(125)I](17a*) and [(125)I]IUdR were evaluated in a model of melanoma B16F0-bearing mice. The pharmacokinetic profile of [(125)I](17a*) suggests rapid release of the active drug [(125)I]IUdR after i.v. administration of [(125)I](17a*). Preliminary metabolism studies in dedicated compartments (i.e. blood, urine and tumour) yielded results consistent with this hypothesis.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Prodrugs / Melanoma Limits: Animals / Humans Language: En Journal: Eur J Med Chem Year: 2016 Document type: Article Affiliation country: France
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Prodrugs / Melanoma Limits: Animals / Humans Language: En Journal: Eur J Med Chem Year: 2016 Document type: Article Affiliation country: France