5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.
Article Details
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Zhi L, Tegley CM, Pio B, Edwards JP, Motamedi M, Jones TK, Marschke KB, Mais DE, Risek B, Schrader WT
5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.
J Med Chem. 2003 Sep 11;46(19):4104-12.
- PubMed ID
- 12954062 [ View in PubMed]
- Abstract
A series of 5-benylidene-1,2-dihydrochromeno[3,4-f]quinolines (4) were synthesized and tested in bioassays to evaluate their progestational activities, receptor- and tissue-selectivity profiles as selective progesterone receptor modulators (SPRMs). Most of the new analogues exhibited as highly potent progestins with more than 100-fold receptor selectivity over other steroid hormone receptors and LG120920 (7b) demonstrated tissue selectivity toward uterus and vagina versus breasts in a rodent model after oral administration.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Medroxyprogesterone acetate Progesterone receptor Ki (nM) 0.34 N/A N/A Details Medroxyprogesterone acetate Progesterone receptor EC 50 (nM) 0.15 N/A N/A Details Medroxyprogesterone acetate Progesterone receptor EC 50 (nM) 0.33 N/A N/A Details Progesterone Androgen receptor IC 50 (nM) 37 N/A N/A Details Progesterone Androgen receptor Ki (nM) 8.5 N/A N/A Details Progesterone Glucocorticoid receptor IC 50 (nM) >1000 N/A N/A Details Progesterone Glucocorticoid receptor Ki (nM) 30.5 N/A N/A Details Progesterone Mineralocorticoid receptor IC 50 (nM) 14 N/A N/A Details Progesterone Progesterone receptor Ki (nM) 3.5 N/A N/A Details Progesterone Progesterone receptor EC 50 (nM) 2.9 N/A N/A Details Progesterone Progesterone receptor EC 50 (nM) 1.8 N/A N/A Details