New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles.
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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.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Mifepristone Progesterone receptor IC 50 (nM) 0.1 N/A N/A Details