Comparison of 2-phenylspiroindenes and 2-phenylspiroindenediones as estrogen receptor ligands--modeling and binding data don't agree!
A series of 2-phenylspiroindenediones was prepared. The spiroindenediones were found to be less active than the corresponding spiroindenes as estrogen receptor ligands and failed to demonstrate the receptor subtype selectivity that had been anticipated from molecular modeling.
Merck Research Laboratories, RY800-B116, PO Box 2000, Rahway, NJ 07065, USA. tim_blizzard@merck.com
Timothy A
TA
Blizzard
Ralph T
RT
Mosley
Elizabeth T
ET
Birzin
Wanda
W
Chan
Milton L
ML
Hammond
D001665:Binding Sites; D006801:Humans; D007192:Indenes / Q000737:chemistry* / Q000378:metabolism*; D008024:Ligands; D008956:Models, Chemical; D008958:Models, Molecular; D011485:Protein Binding; D011960:Receptors, Estrogen / Q000378:metabolism*; D013141:Spiro Compounds / Q000737:chemistry* / Q000378:metabolism*
C476325:2-Phenylspiroindene; D007192:Indenes; D008024:Ligands; D011960:Receptors, Estrogen; D013141:Spiro Compounds