5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.
Article Details
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Zhi L, Tegley CM, Edwards JP, West SJ, Marschke KB, Gottardis MM, Mais DE, Jones TK
5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.
Bioorg Med Chem Lett. 1998 Dec 1;8(23):3365-70.
- PubMed ID
- 9873735 [ View in PubMed]
- Abstract
A series of nonsteroidal human progesterone receptor (hPR) agonists, 5-alkyl 1,2-dihydrochromeno[3,4-f]quinolines, was synthesized and evaluated in cotransfection and competitive receptor binding assays. The 5-alkyl substitution was shown to be responsible for the agonist activity and substitution at C9 dramatically enhanced the potency. A number of analogues in this series showed activities similar to or better than progesterone in the cotransfection and binding assays and analogue 15 exhibited similar in vivo activity as medroxyprogesterone acetate (MPA) in murine uterine wet weight/mammary gland morphology assays.
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) >10000 N/A N/A Details Progesterone Androgen receptor Ki (nM) 8.5 N/A N/A Details Progesterone Glucocorticoid receptor Ki (nM) 30.5 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) >10000 N/A N/A Details