Title of article
Synthesis and biological evaluation of novel thio-substituted chromanes as high-affinity partial agonists for the estrogen receptor
Author/Authors
Lise B. Christiansen، نويسنده , , Martin Wenckens، نويسنده , , Paul S. Bury، نويسنده , , Birgitte Gissel، نويسنده , , Birgit S. Hansen، نويسنده , , Susan M. Thorpe، نويسنده , , Poul Jacobsen، نويسنده , , Anders Kanstrup، نويسنده , , Anker S. J?rgensen، نويسنده , , Lars N?rum، نويسنده , , Karsten Wassermann، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2002
Pages
3
From page
17
To page
19
Abstract
Synthesis of (±)-cis-7-hydroxy-3-phenyl-4-(4-(2-piperidinoethanethio)phenyl)chromane (13) and (±)-cis-7-hydroxy-3-phenyl-4-(4-(2-pyrrolidinoethanethio)phenyl)chromane (15) is presented. These compounds are representatives of a novel class of compounds with high in vitro binding affinity for the estrogen receptor (IC50=7–10 nM), and very low in vitro uterotrophic activity (max stim.=5–17% rel to moxestrol; EC50=0.5–1.8 nM).
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2002
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
791879
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