In:
Organic & Biomolecular Chemistry, Royal Society of Chemistry (RSC), Vol. 21, No. 15 ( 2023), p. 3090-3095
Kurzfassung:
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.
Materialart:
Online-Ressource
ISSN:
1477-0520
,
1477-0539
Sprache:
Englisch
Verlag:
Royal Society of Chemistry (RSC)
Publikationsdatum:
2023
ZDB Id:
2097583-1