Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
We report the discovery of a novel class of glucocorticoid receptor (GR) antagonists based on the chromene molecular scaffold. The compounds exhibit good functional potency and an improved receptor selectivity profile for GR over other steroid receptors when compared to the classical steroidal GR-antagonist, RU-486.
Akritopoulou-Zanze
Irini
I
Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60044, USA. irini.zanze.@abbott.com
Patel
Jyoti R
JR
Hartandi
Kresna
K
Brenneman
Jehrod
J
Winn
Martin
M
Pratt
John K
JK
Grynfarb
Marlene
M
Goos-Nisson
Annika
A
Von Geldern
Thomas W
TW
Kym
Philip R
PR
D001578:Benzopyrans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D015735:Mifepristone / Q000494:pharmacology; D011965:Receptors, Glucocorticoid / Q000037:antagonists & inhibitors*
C412074:5,7-dimethoxy-2-methyl-2H-benzopyran; D001578:Benzopyrans; D011965:Receptors, Glucocorticoid; D015735:Mifepristone