A novel estrogen receptor ligand template.
Three synthetic routes towards a novel estrogen receptor ligand template based on a rigid bicyclo-[3.3.1]-nonene core have been investigated. The prototype compound exhibits potent binding at the ERbeta receptor and promising estrogen receptor subtype selectivity.
Sibley
Robert
R
Bayer Research Center, Bayer Corporation, Pharmaceutical Division, 400 Morgan Lane, West Haven, CT 06516, USA. robert.sibley.b@bayer.com
Hatoum-Mokdad
Holia
H
Schoenleber
Robert
R
Musza
Laszlo
L
Stirtan
William
W
Marrero
Diana
D
Carley
William
W
Xiao
Hong
H
Dumas
Jacques
J
D000475:Alkenes / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology; D045744:Cell Line, Tumor; D004958:Estradiol / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D008565:Membrane Proteins / Q000819:agonists / Q000378:metabolism; D053766:Presenilin-2; D020849:Raloxifene Hydrochloride / Q000494:pharmacology; D011960:Receptors, Estrogen / Q000037:antagonists & inhibitors / Q000378:metabolism*
D000475:Alkenes; D019086:Bridged Bicyclo Compounds, Heterocyclic; D008024:Ligands; D008565:Membrane Proteins; C508861:PSEN2 protein, human; D053766:Presenilin-2; D011960:Receptors, Estrogen; D020849:Raloxifene Hydrochloride; D004958:Estradiol