Abstract
In the course of our studies on retinoic acid receptor (RAR) agonists, we have designed and synthesized a series of quinoxaline derivatives. One of them, 4-[5-(5,6,7,8-tetrahydro-5,5,8, 8-tetramethyl-2-quinoxalinyl)-1H-2-pyrrolyl]benzoic acid (3a), which possesses a 2,5-disubstituted pyrrole moiety, showed selectivity for the RARalpha receptor and exerted highly potent cell-differentiating activity on HL-60 cells.
MeSH terms
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Benzoates / chemical synthesis*
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Benzoates / chemistry
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Benzoates / metabolism
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Benzoates / pharmacology
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Binding, Competitive
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Cell Differentiation / drug effects
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Cell Line
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Humans
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Quinoxalines / chemical synthesis*
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Quinoxalines / chemistry
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Quinoxalines / metabolism
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Quinoxalines / pharmacology
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Receptors, Retinoic Acid / agonists*
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Receptors, Retinoic Acid / metabolism
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Retinoic Acid Receptor alpha
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Retinoids / chemical synthesis*
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Retinoids / chemistry
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Retinoids / metabolism
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Retinoids / pharmacology
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Structure-Activity Relationship
Substances
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Benzoates
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Quinoxalines
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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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Retinoids
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ER 34617