Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands.
A series of ligands with varying heterocyclic cores and substituents that display a range of selectivity's (up to >100x) for ER-beta over ER-alpha are reported.
Chesworth
Richard
R
Cardiovascular and Metabolic Diseases, Medicinal Chemistry, Pfizer Global Research and Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA. rchesworth@gmail.com
Wessel
Matthew D
MD
Heyden
Lisa
L
Mangano
F Michael
FM
Zawistoski
Michael
M
Gegnas
Laura
L
Galluzzo
David
D
Lefker
Bruce
B
Cameron
Kimberly O
KO
Tickner
Jeanne
J
Lu
Bihong
B
Castleberry
Tessa A
TA
Petersen
Donna N
DN
Brault
Amy
A
Perry
Pia
P
Ng
Oicheng
O
Owen
Thomas A
TA
Pan
Lydia
L
Ke
Hua-Zhu
HZ
Brown
Thomas A
TA
Thompson
David D
DD
DaSilva-Jardine
Paul
P
D045744:Cell Line, Tumor; D018360:Crystallography, X-Ray; D047628:Estrogen Receptor alpha / Q000378:metabolism; D047629:Estrogen Receptor beta / Q000737:chemistry / Q000378:metabolism*; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D006801:Humans; D007202:Indicators and Reagents; D007700:Kinetics; D008024:Ligands; D020845:Selective Estrogen Receptor Modulators / Q000737:chemistry; D013329:Structure-Activity Relationship
D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D006571:Heterocyclic Compounds; D007202:Indicators and Reagents; D008024:Ligands; D020845:Selective Estrogen Receptor Modulators