Identification of highly potent retinoic acid receptor α-selective antagonists

…, AT Johnson, ES Klein, L Wang, B Khalifa…

文献索引：Teng, Min; Duong, Tien T.; Johnson, Alan T.; Klein, Elliott S.; Wang, Liming; Khalifa, Berket; Chandraratna, Roshantha A. S. Journal of Medicinal Chemistry, 1997 , vol. 40, # 16 p. 2445 - 2451

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被引用次数: 57

摘要

The syntheses and full retinoid receptor characterization of a novel series of retinoic acid receptor α (RARα) antagonists, 1-5, are described. These compounds bind with high affinity to RARα but were completely inactive in gene transactivation. They were also potent and effective antagonists of retinoic acid (RA) induced gene transcription at RARα. Compounds 1-5 exhibited varying degrees of selectivity for RARα relative to RARβ/γ, with compound 5 ...