New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles.

Article Details

Citation

Fensome A, Bender R, Cohen J, Collins MA, Mackner VA, Miller LL, Ullrich JW, Winneker R, Wrobel J, Zhang P, Zhang Z, Zhu Y

New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles.

Bioorg Med Chem Lett. 2002 Dec 2;12(23):3487-90.

PubMed ID
12419390 [ View in PubMed
]
Abstract

A new series of 3,3-disubstituted-5-aryloxindoles has been synthesized and evaluated for progesterone receptor antagonist (PR) activity in a T47D cell alkaline phosphatase assay and for their ability to bind PR in competition binding studies. In this communication, the synthesis and structure-activity relationships (SARs) of various 3,3-substituents are discussed where it is clear that small alkyl and spiroalkyl groups are required to achieve better PR antagonist activity.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
MifepristoneProgesterone receptorIC 50 (nM)0.1N/AN/ADetails