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

被引：69
作者：
Fensome, A
Bender, R
Cohen, J
Collins, MA
Mackner, VA
Miller, LL
Ullrich, JW
Winneker, R
Wrobel, J
Zhang, PW
Zhang, ZM
Zhu, Y
机构：
[1] Wyeth Ayerst Res, Chem Sci, Collegeville, PA 19426 USA
[2] Wyeth Ayerst Res, Womens Hlth Res Inst, Collegeville, PA 19426 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 23期
关键词：
D O I：
10.1016/S0960-894X(02)00746-1
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A neck 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 structurc-activiy 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. (C) 2002 Elsevier Science Ltd. All rights reserved.
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收藏
页码：3487 / 3490
页数：4
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