title: Optimization and metabolic stabilization of a class of nonsteroidal glucocorticoid modulators.
abstract: The optimization of a series of nonsteroidal glucocorticoid modulators is reported. Potent selective GR ligands that have improved metabolic stability were discovered typified by the subnanomolar acid 12 (GR binding IC(50)=0.6 nM).
authors.affiliation: Metabolic Disease Research, Abbott Laboratories, Dept 4CB, Bldg. AP-10, Rm. L-14, 100 Abbott Park Road, Abott Park, IL 60064-6098, USA. james.link@abbott.com
authors.forename: J T
authors.initials: JT
authors.lastname: Link
authors.forename: Bryan K
authors.initials: BK
authors.lastname: Sorensen
authors.forename: Jyoti
authors.initials: J
authors.lastname: Patel
authors.forename: David
authors.initials: D
authors.lastname: Arendsen
authors.forename: Gaoquan
authors.initials: G
authors.lastname: Li
authors.forename: Susan
authors.initials: S
authors.lastname: Swanson
authors.forename: Bach
authors.initials: B
authors.lastname: Nguyen
authors.forename: Maurice
authors.initials: M
authors.lastname: Emery
authors.forename: Marlena
authors.initials: M
authors.lastname: Grynfarb
authors.forename: Annika
authors.initials: A
authors.lastname: Goos-Nilsson
mesh_terms: D006801:Humans; D008024:Ligands; D011485:Protein Binding; D011965:Receptors, Glucocorticoid / Q000187:drug effects* / Q000378:metabolism
chemical_list: D008024:Ligands; D011965:Receptors, Glucocorticoid