Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
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Jiang W, Fiordeliso JJ, Allan G, Linton O, Tannenbaum P, Xu J, Zhu P, Gunnet J, Demarest K, Lundeen S, Sui Z
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist.
Bioorg Med Chem Lett. 2007 Mar 1;17(5):1471-4. Epub 2006 Oct 5.
- PubMed ID
- 17258455 [ View in PubMed]
- Abstract
Mifepristone is a non-selective antagonist of 3-oxosteroid receptors with both abortifacient and anti-diabetic activities. For glucocorticoid receptor (GR) program, we sought an unexplored, synthetically accessible phosphorus-containing steroidal mimetic of mifepristone, suitable for parallel synthesis of analogues. One compound 4a, with high oral bioavailability (59%) in rat, exhibited functional antagonism of GR in oral glucose tolerance test (OGTT). Thus this series of compounds might be potentially useful for the treatment of type II diabetes.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Mifepristone Glucocorticoid receptor Ki (nM) 1 N/A N/A Details Mifepristone Progesterone receptor IC 50 (nM) 2.6 N/A N/A Details