Abstract
Synthesis and structure-activity relationship of RXR antagonists employing a diazepinylbenzoic acid scaffold are described. Of those antagonists, sulfonamide derivatives (6v and 6w) reveal a high antagonistic activity and good pharmacokinetic properties.
MeSH terms
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Administration, Oral
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Benzoates / chemical synthesis*
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Benzoates / chemistry*
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Biphenyl Compounds / chemical synthesis*
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Biphenyl Compounds / chemistry*
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Humans
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Inhibitory Concentration 50
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Models, Chemical
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Molecular Structure
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Receptors, Retinoic Acid / antagonists & inhibitors*
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Receptors, Retinoic Acid / chemistry*
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Retinoic Acid Receptor alpha
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Structure-Activity Relationship
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Time Factors
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Trans-Activators
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Transcription Factors / chemistry
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Transcriptional Activation
Substances
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Benzoates
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Biphenyl Compounds
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RARA protein, human
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Receptors, Retinoic Acid
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Retinoic Acid Receptor alpha
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Trans-Activators
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Transcription Factors
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diazepinylbenzoic acid