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.
Blizzard
Timothy A
TA
Merck Research Laboratories, RY800-B116, PO Box 2000, Rahway, NJ 07065, USA. tim_blizzard@merck.com
Mosley
Ralph T
RT
Birzin
Elizabeth T
ET
Chan
Wanda
W
Hammond
Milton L
ML
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