Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
Article Details
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Akritopoulou-Zanze I, Patel JR, Hartandi K, Brenneman J, Winn M, Pratt JK, Grynfarb M, Goos-Nisson A, Von Geldern TW, Kym PR
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
Bioorg Med Chem Lett. 2004 May 3;14(9):2079-82.
- PubMed ID
- 15080982 [ View in PubMed]
- Abstract
We report the discovery of a novel class of glucocorticoid receptor (GR) antagonists based on the chromene molecular scaffold. The compounds exhibit good functional potency and an improved receptor selectivity profile for GR over other steroid receptors when compared to the classical steroidal GR-antagonist, RU-486.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Mifepristone Glucocorticoid receptor IC 50 (nM) 5 N/A N/A Details Mifepristone Glucocorticoid receptor IC 50 (nM) 1 N/A N/A Details Mifepristone Progesterone receptor IC 50 (nM) 3 N/A N/A Details