Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes

Ulrich Schopfer; Philippe Schoeffter; Serge F Bischoff; Joachim Nozulak; Dominik Feuerbach; Philipp Floersheim

doi:10.1021/jm015577l

Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes

J Med Chem. 2002 Mar 28;45(7):1399-401. doi: 10.1021/jm015577l.

Authors

Ulrich Schopfer, Philippe Schoeffter, Serge F Bischoff, Joachim Nozulak, Dominik Feuerbach, Philipp Floersheim

PMID: 11906280
DOI: 10.1021/jm015577l

Abstract

In an effort to identify selective ligands for the estrogen receptor subtype ERbeta, a series of aryl benzthiophenes was synthesized. In a radioligand binding assay and reporter gene assays in HeLa and SH-SY5Y cells, compounds were characterized as ERbeta-selective agonists. By targeting ERbeta in the brain, these compounds could lead to drugs able to separate the beneficial effects of estrogens on mood, learning, and memory from side effects such as the stimulation of endometrial and breast cancer.

Publication types

Letter

MeSH terms

Amino Acid Motifs
Binding Sites
Central Nervous System Diseases / drug therapy
Central Nervous System Diseases / metabolism*
Crystallography, X-Ray
Estrogen Receptor beta
HeLa Cells
Humans
Ligands
Models, Chemical
Models, Molecular
Protein Structure, Tertiary
Receptors, Estrogen / agonists*
Receptors, Estrogen / chemistry
Thiophenes / chemistry*
Thiophenes / pharmacology*
Tumor Cells, Cultured

Substances

Estrogen Receptor beta
Ligands
Receptors, Estrogen
Thiophenes
benzothiophene