2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs).
A series of 2-phenylspiroindenes was prepared. The most active analogue (2) was found to be comparable in potency to raloxifene (1) as an estrogen receptor ligand.
Blizzard
Timothy A
TA
Merck Research Laboratories, RY800-B116, PO Box 2000, Rahway, NJ 07065, USA. tim_blizzard@merck.com
Morgan
Jerry D
JD
Mosley
Ralph T
RT
Birzin
Elizabeth T
ET
Frisch
Katalin
K
Rohrer
Susan P
SP
Hammond
Milton L
ML
D000478:Alkylation; D000818:Animals; D001894:Borohydrides; D018360:Crystallography, X-Ray; D006801:Humans; D066298:In Vitro Techniques; D007192:Indenes / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D020849:Raloxifene Hydrochloride / Q000494:pharmacology; D051381:Rats; D011960:Receptors, Estrogen / Q000187:drug effects; D020845:Selective Estrogen Receptor Modulators / Q000138:chemical synthesis* / Q000494:pharmacology*; D013141:Spiro Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
C476325:2-Phenylspiroindene; D001894:Borohydrides; D007192:Indenes; D007202:Indicators and Reagents; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators; D013141:Spiro Compounds; D020849:Raloxifene Hydrochloride; C025364:sodium borohydride