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, 12 (1), 17-9

Synthesis and Biological Evaluation of Novel Thio-Substituted Chromanes as High-Affinity Partial Agonists for the Estrogen Receptor

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Synthesis and Biological Evaluation of Novel Thio-Substituted Chromanes as High-Affinity Partial Agonists for the Estrogen Receptor

Lise B Christiansen et al. Bioorg Med Chem Lett.

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 (IC(50)=7-10 nM), and very low in vitro uterotrophic activity (max stim.=5-17% rel to moxestrol; EC(50)=0.5-1.8 nM).

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