5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.

Article Details

Citation

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
DrugTargetPropertyMeasurementpHTemperature (°C)
Medroxyprogesterone acetateProgesterone receptorKi (nM)0.34N/AN/ADetails
Medroxyprogesterone acetateProgesterone receptorEC 50 (nM)0.15N/AN/ADetails
Medroxyprogesterone acetateProgesterone receptorEC 50 (nM)>10000N/AN/ADetails
ProgesteroneAndrogen receptorKi (nM)8.5N/AN/ADetails
ProgesteroneGlucocorticoid receptorKi (nM)30.5N/AN/ADetails
ProgesteroneProgesterone receptorKi (nM)3.5N/AN/ADetails
ProgesteroneProgesterone receptorEC 50 (nM)2.9N/AN/ADetails
ProgesteroneProgesterone receptorEC 50 (nM)>10000N/AN/ADetails