Tetrahydrofluorenones with conformationally restricted side chains as selective estrogen receptor beta ligands.
A series of 2-9a bridged tetrahydrofluorenone derivatives were prepared which exhibited significant binding affinity for ERbeta and were highly selective.
Wildonger
Kenneth J
KJ
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. ken_wildonger@merck.com
Ratcliffe
Ronald W
RW
Mosley
Ralph T
RT
Hammond
Milton L
ML
Birzin
Elizabeth T
ET
Rohrer
Susan P
SP
D047629:Estrogen Receptor beta / Q000737:chemistry* / Q000378:metabolism*; D005449:Fluorenes / Q000138:chemical synthesis / Q000737:chemistry*; D006801:Humans; D006859:Hydrogen / Q000737:chemistry*; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D008968:Molecular Conformation
D047629:Estrogen Receptor beta; D005449:Fluorenes; D008024:Ligands; D006859:Hydrogen