Synthesis and estrogenic activities of novel 7-thiosubstituted estratrienederivatives

Authors
Miller, CP Jirkovsky, I Tran, BD Harris, HA Moran, RA Komm, BS
Citation
Cp. Miller et al., Synthesis and estrogenic activities of novel 7-thiosubstituted estratrienederivatives, BIOORG MED, 10(2), 2000, pp. 147-151
Citations number
21
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
2
Year of publication
2000
Pages
147 - 151
Database
ISI
SICI code
0960-894X(20000117)10:2<147:SAEAON>2.0.ZU;2-3
Abstract
A diastereomerically pure series of 7 alpha-thioestratrienes was prepared a nd evaluated for its affinity for both the human estrogen receptor alpha an d the more recently discovered estrogen receptor beta. The functional estro genic activities of the compounds were measured in a MCF-7 ERE-tk-luciferas e assay. The activities and selectivities of the compounds were sensitive t o the nature of the thioether side chain. (C) 2000 Elsevier Science Ltd. Al l rights reserved.