Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent,orally active progesterone receptor agonists |
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Authors: | Fensome Andrew Koko Marci Wrobel Jay Zhang Puwen Zhang Zhiming Cohen Jeffrey Lundeen Scott Rudnick Kelly Zhu Yuan Winneker Richard |
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Institution: | Chemical Sciences, Wyeth Research, Collegeville, PA 19426, USA. fensoma@wyeth.com |
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Abstract: | During the course of our studies on 3,3-disubstituted-5-aryloxindoles derived progesterone receptor (PR) antagonists we discovered that changing the amide funtionality to a thio-amide resulted in compounds displaying potent PR agonist activity. In this communication, the synthesis, structure activity relationships (SAR) and in vivo activity of various 5-arylthio-oxindoles will be discussed. |
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