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Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists
Authors:Richards Steven J  von Geldern Thomas W  Jacobson Peer  Wilcox Denise  Nguyen Phong  Ohman Lars  Osterlund Marie  Gelius Birgitta  Grynfarb Marlena  Goos-Nilsson Annika  Wang Jiahong  Fung Steven  Kalmanovich Masha
Affiliation:Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA. steven.richards@abbott.com
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.
Keywords:
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