Billaud, Emilie M. F.’s team published research in European Journal of Medicinal Chemistry in 2015-03-06 | CAS: 153034-78-7

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 153034-78-7 belongs to class iodides-buliding-blocks, name is 2-Fluoro-3-iodo-5-methylpyridine, and the molecular formula is C6H5FIN, Formula: C6H5FIN.

Billaud, Emilie M. F. published the artcileSynthesis, radiolabeling and preliminary in vivo evaluation of multimodal radiotracers for PET imaging and targeted radionuclide therapy of pigmented melanoma, Formula: C6H5FIN, the main research area is radiolabeling radiotracer preparation PET imaging radiotherapy melanoma; Fluorine-18; In vivo screening; Iodine-125; Melanoma; PET imaging.

Melanin pigment represents an attractive target to address specific treatment to melanoma cells, such as cytotoxic radionuclides. However, less than half of the patients have pigmented metastases. Hence, specific marker is required to stratify this patient population before proceeding with melanin-targeted radionuclide therapy. In such a context, we developed fluorinated analogs of a previously studied melanin-targeting ligand, N-(2-diethylaminoethyl)-6-iodoquinoxaline-2-carboxamide (ICF01012). These latter can be labeled either with 18F or 131I/125I for positron emission tomog. imaging (melanin-pos. patient selection) and targeted radionuclide therapy purposes. Here we describe the syntheses, radiosyntheses and preclin. evaluations on melanoma-bearing mice model of several iodo- and fluoro(hetero)aromatic derivatives of the ICF01012 scaffold. After preliminary planar gamma scintigraphic and positron emission tomog. imaging evaluations, [125I]- and [18F]-N-[2-(diethylamino)ethyl]-4-fluoro-3-iodobenzamides ([125I]4, [18F]4) were chem. and biol. stable with quite similar tumor uptakes at 1 h p.i. (9.7±2.6% ID/g and 6.8±1.9% ID/g, resp.).

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 153034-78-7 belongs to class iodides-buliding-blocks, name is 2-Fluoro-3-iodo-5-methylpyridine, and the molecular formula is C6H5FIN, Formula: C6H5FIN.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com