Abstract
| - The syntheses and full retinoid receptor characterization of anovel series of retinoic acidreceptor α (RARα) antagonists, 1−5, aredescribed. These compounds bind with high affinityto RARα but were completely inactive in gene transactivation.They were also potent andeffective antagonists of retinoic acid (RA) induced gene transcriptionat RARα. Compounds1−5 exhibited varying degrees of selectivityfor RARα relative to RARβ/γ, with compound5being the most selective in both binding and functional antagonismassays. These compoundswill be invaluable tools in delineating the physiological roles ofRARα in development and inthe adult animal and may themselves be useful therapeutic agents inhuman diseases associatedwith RARα.
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