Synthesis, radiolabeling and preliminary in vivo evaluation of multimodal radiotracers for PET imaging and targeted radionuclide therapy of pigmented melanoma
作者: Emilie M.F. BillaudAurélie Maisonial-BessetLatifa Rbah-VidalAurélien VidalSophie BesseJean-Baptiste BéquignatCaroline DecombatFrançoise DegoulLaurent AudinJean-Bernard DeloyeFrédéric DolléBertrand KuhnastJean-Claude MadelmontSébastien TarritMarie-Josèphe GalmierMichèle BorelPhilippe AuzelouxElisabeth Miot-NoiraultJean-Michel Chezal
作者单位: 1Clermont Université, Université d'Auvergne, Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63000 Clermont-Ferrand, France
2Inserm, U 990, F-63000 Clermont-Ferrand, France
3Centre Jean Perrin, F-63011 Clermont-Ferrand, France
4Laboratoires CYCLOPHARMA, Biopôle Clermont-Limagne, Saint-Beauzire F-63360, France
5CEA, Service Hospitalier Frédéric Joliot, F-91406 Orsay, France
刊名: European Journal of Medicinal Chemistry, 2015, Vol.92 , pp.818-838
来源数据库: Elsevier Journal
DOI: 10.1016/j.ejmech.2015.01.034
关键词: MelanomaIn vivo screeningPET imagingIodine-125Fluorine-18
英文摘要: Abstract(#br)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 analogues of a previously studied melanin-targeting ligand, N -(2-diethylaminoethyl)-6-iodoquinoxaline-2-carboxamide ( ICF01012 ). These latter can be labeled either with 18 F or 131 I/ 125 I for positron emission tomography imaging (melanin-positive patient selection) and targeted radionuclide therapy purposes. Here we describe the syntheses, radiosyntheses and preclinical evaluations on melanoma-bearing...
全文获取路径: Elsevier  (合作)
影响因子:3.499 (2012)

  • radionuclide 放射性核素
  • imaging 图像形成
  • multimodal 多峰
  • preliminary 初步
  • targeted 对准目标的
  • pigmented 着色的
  • melanoma 黑瘤
  • PET PagE frame Table
  • therapy 治疗
  • evaluation 评价