Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
A series of potent steroidal glucocorticoid receptor antagonists has been discovered. After conjugation to cholic acid, the compounds retained an affinity for GR in vitro and had modest in vivo efficacy.
Richards
Steven J
SJ
Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA. steven.richards@abbott.com <steven.richards@abbott.com>
von Geldern
Thomas W
TW
Jacobson
Peer
P
Wilcox
Denise
D
Nguyen
Phong
P
Ohman
Lars
L
Osterlund
Marie
M
Gelius
Birgitta
B
Grynfarb
Marlena
M
Goos-Nilsson
Annika
A
Wang
Jiahong
J
Fung
Steven
S
Kalmanovich
Masha
M
D000818:Animals; D001647:Bile Acids and Salts / Q000737:chemistry*; D006801:Humans; D008861:Microsomes / Q000187:drug effects / Q000378:metabolism; D015394:Molecular Structure; D051381:Rats; D011965:Receptors, Glucocorticoid / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
D001647:Bile Acids and Salts; D011965:Receptors, Glucocorticoid