Synthesis, radioiodination and in vivo screening of novel potent iodinated and fluorinated radiotracers as melanoma imaging and therapeutic probes

Autor: Janine Papon, Philippe Auzeloux, Jean-Michel Chezal, Aurélie Maisonial, Latifa Rbah-Vidal, Michèle Borel, Marie-Josèphe Galmier, Serge Askienazy, Martine Bayle, Sébastien Tarrit, Emilie M. F. Billaud, Elisabeth Miot-Noirault, Nicole Moins, Jean-Claude Madelmont, Sophie Besse, Laurent Audin
Přispěvatelé: Imagerie Moléculaire et Stratégies Théranostiques (IMoST), Institut National de la Santé et de la Recherche Médicale (INSERM)-Université Clermont Auvergne [2017-2020] (UCA [2017-2020]), Imagerie Moléculaire et Thérapie Vectorisée (IMTV), ITMO ' Technologies pour la Santé '-Cancéropôle CLARA-Institut National de la Santé et de la Recherche Médicale (INSERM)-Université d'Auvergne - Clermont-Ferrand I (UdA), Etude Métabolique des Molécules Marquées, Université d'Auvergne - Clermont-Ferrand I (UdA)-Institut National de la Santé et de la Recherche Médicale (INSERM), Centre Jean Perrin [Clermont-Ferrand] (UNICANCER/CJP), UNICANCER
Jazyk: angličtina
Rok vydání: 2013
Předmět:
Male
Time Factors
Halogenation
[SDV]Life Sciences [q-bio]
Targeted radionuclide therapy
Melanoma
Experimental
[SDV.CAN]Life Sciences [q-bio]/Cancer
01 natural sciences
Iodine Radioisotopes
Mice
03 medical and health sciences
0302 clinical medicine
In vivo
Cell Line
Tumor
Spect imaging
Labelling
Drug Discovery
medicine
Animals
[CHIM]Chemical Sciences
Tissue Distribution
ComputingMilieux_MISCELLANEOUS
Tomography
Emission-Computed
Single-Photon
Pharmacology
Molecular Structure
medicine.diagnostic_test
010405 organic chemistry
Chemistry
business.industry
[CHIM.ORGA]Chemical Sciences/Organic chemistry
Melanoma
Organic Chemistry
General Medicine
Pet imaging
medicine.disease
0104 chemical sciences
3. Good health
Mice
Inbred C57BL
Models
Chemical
Positron emission tomography
030220 oncology & carcinogenesis
Benzamides
Nuclear medicine
business
[CHIM.RADIO]Chemical Sciences/Radiochemistry
Emission computed tomography
Zdroj: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, Elsevier, 2013, 63, pp.840-853. ⟨10.1016/j.ejmech.2012.11.047⟩
ISSN: 0223-5234
1768-3254
Popis: 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 [125I]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 [131I]-labelled analogues were generally higher than 100 cGy/MBq injected (98.9–150.5 cGy/MBq for [131I]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.
Databáze: OpenAIRE
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