1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.

Article Details

Citation

Kern JC, Terefenko E, Trybulski E, Berrodin TJ, Cohen J, Winneker RC, Yudt MR, Zhang Z, Zhu Y, Zhang P

1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4816-8. doi: 10.1016/j.bmcl.2010.06.109. Epub 2010 Jun 25.

PubMed ID
20638844 [ View in PubMed
]
Abstract

Non-steroidal 1-methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalenes and acyclic derivatives were evaluated as novel series of progesterone receptor (PR) antagonists using the T47D cell alkaline phosphatase assay. Moderate to potent PR antagonists were achieved with these scaffolds. Several compounds (e.g., 15 and 20) demonstrated low nanomolar PR antagonist potency and good selectivity versus other steroid receptors.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
MifepristoneGlucocorticoid receptorIC 50 (nM)0.6N/AN/ADetails
MifepristoneProgesterone receptorIC 50 (nM)0.2N/AN/ADetails