Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists.
Two series of 6-hydroxy and 7-hydroxy tetrahydroisoquinolines were prepared. Evaluating a range of C-1, C-4, and N-substituents led to the discovery of ER alpha and ER beta selective analogs.
Chesworth
Richard
R
Pfizer Global Research and Development, CVMD Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA. richard_chesworth@groton.pfizer.com
Zawistoski
Michael P
MP
Lefker
Bruce A
BA
Cameron
Kimberly O
KO
Day
Robert F
RF
Mangano
F Michael
FM
Rosati
Robert L
RL
Colella
Stacy
S
Petersen
Donna N
DN
Brault
Amy
A
Lu
Bihong
B
Pan
Lydia C
LC
Perry
Pia
P
Ng
Oicheng
O
Castleberry
Tessa A
TA
Owen
Thomas A
TA
Brown
Thomas A
TA
Thompson
David D
DD
DaSilva-Jardine
Paul
P
D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D047628:Estrogen Receptor alpha / Q000737:chemistry; D047629:Estrogen Receptor beta / Q000737:chemistry; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D011485:Protein Binding; D020845:Selective Estrogen Receptor Modulators / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis / Q000494:pharmacology*
D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D008024:Ligands; D020845:Selective Estrogen Receptor Modulators; D044005:Tetrahydroisoquinolines