Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
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Zhi L, Ringgenberg JD, Edwards JP, Tegley CM, West SJ, Pio B, Motamedi M, Jones TK, Marschke KB, Mais DE, Schrader WT
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
Bioorg Med Chem Lett. 2003 Jun 16;13(12):2075-8.
- PubMed ID
- 12781198 [ View in PubMed]
- Abstract
A series of 1,2-dihydrochromeno[3,4-f]quinoline derivatives was synthesized and tested in biological assays to evaluate the nonsteroidal progesterone receptor modulator pharmacophore (4) as antiprogestins. A number of potent analogues were identified by modification of the substituents at the D-ring.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Mifepristone Glucocorticoid receptor IC 50 (nM) 0.8 N/A N/A Details Mifepristone Progesterone receptor Ki (nM) 1.1 N/A N/A Details Mifepristone Progesterone receptor IC 50 (nM) 3.3 N/A N/A Details Mifepristone Progesterone receptor EC 50 (nM) 0.3 N/A N/A Details