Review of fluorescent steroidal ligands for the estrogen receptor 1995–2018

Publication date: April 2019Source: Steroids, Volume 144Author(s): Nisal Gajadeera, Robert N. HansonAbstractThe development of fluorescent ligands for the estrogen receptor (ER) continues to be of interest. Over the past 20 years, most efforts have focused on appending an expanding variety of fluorophores to the B-, C- and D-rings of the steroidal scaffold. This review highlights the synthesis and evaluation of derivatives substituted primarily at the 6-, 7α- and 17α-positions, culminating with our recent work on 11β-substituted estradiols, and proposes an approach to new fluorescent imaging agents that retain high ER affinity.Graphical abstractA comprehensive review of fluorescent derivatives of steroidal ER ligands.
Source: Steroids - Category: Drugs & Pharmacology Source Type: research