Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.

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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
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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
DrugTargetPropertyMeasurementpHTemperature (°C)
MifepristoneGlucocorticoid receptorIC 50 (nM)5N/AN/ADetails
MifepristoneGlucocorticoid receptorIC 50 (nM)1N/AN/ADetails
MifepristoneProgesterone receptorIC 50 (nM)3N/AN/ADetails