放射性碘化雌激素的合成与评估，用于男性泌尿生殖肿瘤的诊断和治疗。
Synthesis and evaluation of radioiodinated estrogens for diagnosis and therapy of male urogenital tumours.
发表日期：2023 Mar 22
作者：
Feodor Braun, Marcel Jaschinski, Philipp Täger, Verena Marmann, Melanie von Brandenstein, Barbara Köditz, Thomas Fischer, Sergio Muñoz-Vázquez, Beate Zimmermanns, Markus Dietlein, Ferdinand Sudbrock, Phillip Krapf, Dietmar Fischer, Axel Heidenreich, Alexander Drzezga, Stefan Kirsch, Markus Pietsch, Klaus Schomäcker
来源：
Cellular & Molecular Immunology
摘要：
本文介绍了24种雌激素制备，它们与雌激素受体（ER）的亲和力以及放射性碘化雌激素与ER阳性的男性膀胱肿瘤细胞（HTB9）的结合研究。利用荧光异向性法选出了亲和力最高的雌激素。在11β位上引入2,2,2-三氟乙基基团，其亲和力尤为显著。对17α-乙烯基进行（放射）碘化。HTB9细胞的结合研究表明，放射性共轭物19和31的皮克摩尔亲和力，表明它们有望成为靶向泌尿生殖肿瘤的有前途的药物。
The preparation of 24 estrogens, their estrogen receptor (ER) affinity and studies of radioiodinated estrogen binding to ER-positive male bladder tumor cells (HTB9) are described. The estrogens with the highest affinity were selected using fluorescence anisotropy assays. A 2,2,2-trifluoroethyl group at the 11β-position caused particularly promising affinity. (Radio)iodination was performed on the 17α-vinyl group. Binding studies on HTB9 cells revealed picomolar affinities of radioconjugates 19 and 31, indicating promising ability for targeting of urogenital tumors.