5-Aryl indanones and derivatives as non-steroidal progesterone receptor modulators

被引：12
|
作者：
Kern, Jeffrey C. [1 ]
Terefenko, Eugene [1 ]
Trybulski, Eugene [1 ]
Berrodin, Thomas J. [2 ]
Cohen, Jeffrey [2 ]
Winneker, Richard C. [2 ]
Yudt, Matthew R. [2 ]
Zhang, Zhiming [2 ]
Zhu, Yuan [2 ]
Zhang, Puwen [1 ]
机构：
[1] Wyeth Ayerst Res, Chem Sci, Collegeville, PA 19426 USA
[2] Wyeth Ayerst Res, Musculoskeletal Biol, Collegeville, PA 19426 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 23期
关键词：
Progesterone receptor; Nuclear receptor; Progesterone receptor agonist; Progesterone receptor antagonist; 5-Aryl indanone; 5-Aryl indan-1-one oxime; 5-Aryl indan-1-ols; MIFEPRISTONE; ANTAGONISTS; POTENT; LIGANDS;
D O I：
10.1016/j.bmcl.2009.10.008
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Novel 5-aryl indanones, inden-1-one oximes, and inden-1-ols were synthesized and evaluated as progesterone receptor (PR) modulators using the T47D cell alkaline phosphatase assay. Both PR agonists and antagonists were achieved with appropriate 3- and 5-substitution from indanones and inden-1-ols while inden-1-one oximes provided only PR antagonists. Several compounds such as 10 and 11 demonstrated potent in vitro PR agonist potency similar to that of steroidal progesterone (1). In addition, a number of compounds (e. g., 12, 13, 17, 18) showed potent PR antagonist activity indicating the indanones and derivatives are promising PR modulator templates. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：6666 / 6669
页数：4
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