Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.

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Du Y, Li Q, Xiong B, Hui X, Wang X, Feng Y, Meng T, Hu D, Zhang D, Wang M, Shen J

Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.

Bioorg Med Chem. 2010 Jun 15;18(12):4255-68. doi: 10.1016/j.bmc.2010.04.092. Epub 2010 May 24.

PubMed ID
20510622 [ View in PubMed
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Abstract

A novel class of non-steroidal progesterone receptor antagonists with aromatic beta-amino-ketone scaffold have been synthesized and characterized with high binding affinity and great selectivity for the cognate receptors. Among them, compound 22 was shown to be the most potent progesterone receptor antagonist in cotransfection assay and a murine model of ligand-induced decidualization.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
MifepristoneGlucocorticoid receptorIC 50 (nM)0.95N/AN/ADetails
MifepristoneGlucocorticoid receptorEC 50 (nM)872N/AN/ADetails
MifepristoneGlucocorticoid receptorKi (nM)0.84N/AN/ADetails
MifepristoneProgesterone receptorIC 50 (nM)0.6N/AN/ADetails
MifepristoneProgesterone receptorEC 50 (nM)>10000N/AN/ADetails
ProgesteroneAndrogen receptorKi (nM)35N/AN/ADetails
ProgesteroneProgesterone receptorIC 50 (nM)>10000N/AN/ADetails
ProgesteroneProgesterone receptorEC 50 (nM)15.2N/AN/ADetails
ProgesteroneProgesterone receptorKi (nM)5.1N/AN/ADetails
StanoloneAndrogen receptorKi (nM)4.7N/AN/ADetails