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

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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