title: Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
abstract: 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.
authors.affiliation: Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60044, USA. irini.zanze.@abbott.com
authors.forename: Irini
authors.initials: I
authors.lastname: Akritopoulou-Zanze
authors.forename: Jyoti R
authors.initials: JR
authors.lastname: Patel
authors.forename: Kresna
authors.initials: K
authors.lastname: Hartandi
authors.forename: Jehrod
authors.initials: J
authors.lastname: Brenneman
authors.forename: Martin
authors.initials: M
authors.lastname: Winn
authors.forename: John K
authors.initials: JK
authors.lastname: Pratt
authors.forename: Marlene
authors.initials: M
authors.lastname: Grynfarb
authors.forename: Annika
authors.initials: A
authors.lastname: Goos-Nisson
authors.forename: Thomas W
authors.initials: TW
authors.lastname: Von Geldern
authors.forename: Philip R
authors.initials: PR
authors.lastname: Kym
mesh_terms: D001578:Benzopyrans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D015735:Mifepristone / Q000494:pharmacology; D011965:Receptors, Glucocorticoid / Q000037:antagonists & inhibitors*
chemical_list: C412074:5,7-dimethoxy-2-methyl-2H-benzopyran; D001578:Benzopyrans; D011965:Receptors, Glucocorticoid; D015735:Mifepristone