Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes.
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.
Schopfer
Ulrich
U
Schoeffter
Philippe
P
Bischoff
Serge F
SF
Nozulak
Joachim
J
Feuerbach
Dominik
D
Floersheim
Philipp
P
D020816:Amino Acid Motifs; D001665:Binding Sites; D002493:Central Nervous System Diseases / Q000188:drug therapy / Q000378:metabolism*; D018360:Crystallography, X-Ray; D047629:Estrogen Receptor beta; D006367:HeLa Cells; D006801:Humans; D008024:Ligands; D008956:Models, Chemical; D008958:Models, Molecular; D017434:Protein Structure, Tertiary; D011960:Receptors, Estrogen / Q000819:agonists* / Q000737:chemistry; D013876:Thiophenes / Q000737:chemistry* / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D047629:Estrogen Receptor beta; D008024:Ligands; D011960:Receptors, Estrogen; D013876:Thiophenes; C088015:benzothiophene