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.
Bayer Research Center, Bayer Corporation, Pharmaceutical Division, 400 Morgan Lane, West Haven, CT 06516, USA. robert.sibley.b@bayer.com
Robert
R
Sibley
Holia
H
Hatoum-Mokdad
Robert
R
Schoenleber
Laszlo
L
Musza
William
W
Stirtan
Diana
D
Marrero
William
W
Carley
Hong
H
Xiao
Jacques
J
Dumas
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