Optimization and metabolic stabilization of a class of nonsteroidal glucocorticoid modulators

The synthesis and biochemical profile of the potent glucocorticoid receptor modulator 12 (h-GR binding IC 50 = 0.6 nm) is reported. The optimization of a series of nonsteroidal glucocorticoid modulators is reported. Potent selective GR ligands that have improved metabolic stability were discovered t...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-08, Vol.14 (16), p.4169-4172
Hauptverfasser:	Link, J.T, Sorensen, Bryan K, Patel, Jyoti, Arendsen, David, Li, Gaoquan, Swanson, Susan, Nguyen, Bach, Emery, Maurice, Grynfarb, Marlena, Goos-Nilsson, Annika
Format:	Artikel
Sprache:	eng
Schlagworte:	Antidiabetic Biological and medical sciences Glucocorticoid modulator Hormones. Endocrine system Humans Ligands Medical sciences Pharmacology. Drug treatments Protein Binding Receptors, Glucocorticoid - drug effects Receptors, Glucocorticoid - metabolism
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Beschreibung
Zusammenfassung:	The synthesis and biochemical profile of the potent glucocorticoid receptor modulator 12 (h-GR binding IC 50 = 0.6 nm) is reported. 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).
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2004.06.023