Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.

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Zhi L, Tegley CM, Pio B, Edwards JP, Jones TK, Marschke KB, Mais DE, Risek B, Schrader WT

Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.

Bioorg Med Chem Lett. 2003 Jun 16;13(12):2071-4.

PubMed ID
12781197 [ View in PubMed
]
Abstract

A series of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives were synthesized and tested in biological assays to evaluate scope and limitations of the nonsteroidal SPRM pharmacophore (3). A number of orally available highly potent nonsteroidal modulators were identified by modification of the substituents at 5-methylidene position.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
MifepristoneProgesterone receptorIC 50 (nM)0.3N/AN/ADetails
MifepristoneProgesterone receptorKi (nM)1.1N/AN/ADetails
ProgesteroneAndrogen receptorIC 50 (nM)37N/AN/ADetails
ProgesteroneGlucocorticoid receptorIC 50 (nM)>1000N/AN/ADetails
ProgesteroneMineralocorticoid receptorIC 50 (nM)14N/AN/ADetails
ProgesteroneProgesterone receptorKi (nM)3.5N/AN/ADetails
ProgesteroneProgesterone receptorEC 50 (nM)2.9N/AN/ADetails