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.
MeSH terms
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Alkaline Phosphatase / biosynthesis
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Animals
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Binding, Competitive / drug effects
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Breast Neoplasms / enzymology
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Decidua / drug effects
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Drug Design
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Female
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Humans
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Indicators and Reagents
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Indoles / chemical synthesis*
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Indoles / pharmacology*
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Medroxyprogesterone Acetate / pharmacology
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Ovariectomy
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Rats
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Receptors, Progesterone / agonists*
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Structure-Activity Relationship
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Thiones / chemical synthesis*
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Thiones / pharmacology*
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Tumor Cells, Cultured
Substances
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Indicators and Reagents
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Indoles
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Receptors, Progesterone
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Thiones
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Medroxyprogesterone Acetate
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Alkaline Phosphatase