Abstract
In the course of studies on novel retinoids, we have designed and synthesized a series of quinoline derivatives. One of them, 4-[5-[8-(1-methylethyl)-4-phenyl-2-quinolinyl]-1H-2-pyrrolyl]benzoic acid (12f) shows potent RARalpha-selective antagonistic activity.
MeSH terms
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Aldehydes / chemical synthesis
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Aldehydes / pharmacology
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Benzoates / chemical synthesis
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Benzoates / pharmacology
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Binding, Competitive / drug effects
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HL-60 Cells
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Humans
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Quinolines / chemical synthesis*
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Quinolines / pharmacology*
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Receptors, Retinoic Acid / antagonists & inhibitors*
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Retinoic Acid Receptor alpha
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Structure-Activity Relationship
Substances
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Aldehydes
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Benzoates
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Quinolines
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RARA protein, human
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Receptors, Retinoic Acid
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Retinoic Acid Receptor alpha