Details

Autor(en) / Beteiligte

• Braun, Feodor
• Jaschinski, Marcel
• Täger, Philipp
• Marmann, Verena
• Brandenstein, Melanie von
• Köditz, Barbara
• Fischer, Thomas
• Muñoz-Vázquez, Sergio
• Zimmermanns, Beate
• Dietlein, Markus
• Sudbrock, Ferdinand
• Krapf, Phillip
• Fischer, Dietmar
• Heidenreich, Axel
• Drzezga, Alexander
• Kirsch, Stefan
• Pietsch, Markus
• Schomäcker, Klaus

Titel

Synthesis and evaluation of radioiodinated estrogens for diagnosis and therapy of male urogenital tumours

Ist Teil von

• Organic & biomolecular chemistry, 2023-04, Vol.21 (15), p.39-395

Ort / Verlag

England: Royal Society of Chemistry

Erscheinungsjahr

2023

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• 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. We identified a new estrogen receptor (ER)-targeting ligand with picomolar affinity serving as vehicle for radioiodines. This ligand is a potential radiotheranostics for ER + male tumours.