High affinity retinoic acid receptor antagonists: analogs of AGN 193109

…, L Wang, SJ Gillett, RAS Chandraratna

文献索引：Johnson, Alan T.; Wang, Liming; Gillett, Samuel J.; Chandraratna, Roshantha A. S. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 4 p. 573 - 576

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被引用次数: 20

摘要

A series of high affinity retinoic acid receptor (RAR) antagonists were prepared based upon the known antagonist AGN 193109 (2). Introduction of various phenyl groups revealed a preference for substitution at the para-position relative to the meta-site. Antagonists with the highest affinities for the RARs possessed hydrophobic groups, however, the presence of polar functionality was also well tolerated.