Abstract
A novel series of steroidal compounds were designed and synthesized with various phosphorus-containing groups on the 17beta-side chain as progesterone receptor antagonists. The structure-activity relationships of these compounds are discussed. Selected compounds were tested in an rat progesterone-sensitive assay. Some of these compounds are more potent than mifepristone, with a better selectivity profile in differentiating progesterone receptor from glucocorticoid receptor.
MeSH terms
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Animals
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Binding Sites
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Cell Line
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Female
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Hormone Antagonists / chemistry*
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Hormone Antagonists / metabolism
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Humans
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Mifepristone / chemistry*
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Mifepristone / metabolism
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Molecular Structure
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Phosphorus / chemistry*
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Progesterone / chemistry
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Progesterone / metabolism
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Rats
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Rats, Sprague-Dawley
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Receptors, Progesterone / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Hormone Antagonists
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Receptors, Progesterone
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Phosphorus
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Mifepristone
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Progesterone