title: Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
abstract: 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.
authors.affiliation: Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA. steven.richards@abbott.com <steven.richards@abbott.com>
authors.forename: Steven J
authors.initials: SJ
authors.lastname: Richards
authors.forename: Thomas W
authors.initials: TW
authors.lastname: von Geldern
authors.forename: Peer
authors.initials: P
authors.lastname: Jacobson
authors.forename: Denise
authors.initials: D
authors.lastname: Wilcox
authors.forename: Phong
authors.initials: P
authors.lastname: Nguyen
authors.forename: Lars
authors.initials: L
authors.lastname: Ohman
authors.forename: Marie
authors.initials: M
authors.lastname: Osterlund
authors.forename: Birgitta
authors.initials: B
authors.lastname: Gelius
authors.forename: Marlena
authors.initials: M
authors.lastname: Grynfarb
authors.forename: Annika
authors.initials: A
authors.lastname: Goos-Nilsson
authors.forename: Jiahong
authors.initials: J
authors.lastname: Wang
authors.forename: Steven
authors.initials: S
authors.lastname: Fung
authors.forename: Masha
authors.initials: M
authors.lastname: Kalmanovich
mesh_terms: 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
chemical_list: D001647:Bile Acids and Salts; D011965:Receptors, Glucocorticoid