Abstract
Synthesis and structure activity relationships (SAR) of RAR alpha-selective agonists are discussed. 4-[5-(5,8-Dimethyl-2H-3-chromenyl)-1H-2-pyrrolyl]benzoic acid (12a), which possesses a flat structural moiety and an oxygen atom at the hydrophobic part, showed highly selective transactivation activity at the RAR alpha receptor.
MeSH terms
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Benzoates / chemical synthesis*
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Benzoates / pharmacology
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Benzopyrans / chemical synthesis*
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Benzopyrans / pharmacology
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Cell Differentiation / drug effects
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HL-60 Cells
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Humans
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Naphthalenes / chemical synthesis*
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Naphthalenes / pharmacology
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Pyrroles / chemical synthesis*
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Pyrroles / pharmacology
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Receptors, Retinoic Acid / agonists*
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Retinoic Acid Receptor alpha
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Structure-Activity Relationship
Substances
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Benzoates
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Benzopyrans
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Naphthalenes
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Pyrroles
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RARA protein, human
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Receptors, Retinoic Acid
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Retinoic Acid Receptor alpha