Abstract
New RXR-selective modulators possessing a 6-fluoro trienoic acid moiety (6Z olefin) or a fluorinated/heterocyclic-substituted benzene core ring, were synthesized in an expedient and selective way. A subset of these compounds was evaluated for their metabolic properties (exposure in IRC male mice) and show a dramatic increase of exposure compared to our reference compound, 3 (LG101506).
MeSH terms
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Animals
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Binding, Competitive
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Cell Line
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Coumarins / chemical synthesis*
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Coumarins / pharmacology*
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Drug Design
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Kinetics
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Male
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Mice
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Receptors, Retinoic Acid / drug effects
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Receptors, Retinoic Acid / physiology*
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Retinoic Acid Receptor alpha
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Retinoic Acid Receptor gamma
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Retinoid X Receptors
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Transcription Factors / drug effects
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Transcription Factors / physiology*
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Tretinoin / pharmacokinetics
Substances
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Coumarins
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Rara protein, mouse
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Receptors, Retinoic Acid
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Retinoic Acid Receptor alpha
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Retinoid X Receptors
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Transcription Factors
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retinoic acid receptor beta
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Tretinoin