Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
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Richards SJ, von Geldern TW, Jacobson P, Wilcox D, Nguyen P, Ohman L, Osterlund M, Gelius B, Grynfarb M, Goos-Nilsson A, Wang J, Fung S, Kalmanovich M
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
Bioorg Med Chem Lett. 2006 Dec 1;16(23):6086-90. Epub 2006 Sep 20.
- PubMed ID
- 16987661 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Mifepristone Glucocorticoid receptor IC 50 (nM) 1.1 N/A N/A Details Mifepristone Glucocorticoid receptor IC 50 (nM) 5 N/A N/A Details