Androstenediol analogs as ER-beta-selective SERMs.
A series of 19-substituted androstenediol derivatives was prepared. Some of the novel analogs were surprisingly potent and selective ligands for ER-beta.
Blizzard
Timothy A
TA
Merck Research Laboratories, PO Box 2000, Rahway NJ 07065, USA. tim_blizzard@merck.com
Gude
Candido
C
Morgan
Jerry D
JD
Chan
Wanda
W
Birzin
Elizabeth T
ET
Mojena
Marina
M
Tudela
Consuelo
C
Chen
Fang
F
Knecht
Kristin
K
Su
Qin
Q
Kraker
Bryan
B
Mosley
Ralph T
RT
Holmes
Mark A
MA
Sharma
Nandini
N
Fitzgerald
Paula M D
PM
Rohrer
Susan P
SP
Hammond
Milton L
ML
D015114:Androstenediol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D047629:Estrogen Receptor beta / Q000187:drug effects*; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D008968:Molecular Conformation; D020845:Selective Estrogen Receptor Modulators / Q000138:chemical synthesis / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D047629:Estrogen Receptor beta; D008024:Ligands; D020845:Selective Estrogen Receptor Modulators; D015114:Androstenediol