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

A Fensome, R Bender, J Cohen, MA Collins…

文献索引：Fensome, Andrew; Bender, Reinhold; Cohen, Jeffrey; Collins, Mark A; Mackner, Valerie A; Miller, Lori L; Ullrich, John W; Winneker, Richard; Wrobel, Jay; Zhang, Puwen; Zhang, Zhiming; Zhu, Yuan Bioorganic and medicinal chemistry letters, 2002 , vol. 12, # 23 p. 3487 - 3490

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被引用次数: 54

摘要

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 ...