Bioorganic and Medicinal Chemistry Letters p. 573 - 576 (1999)
Update date:2022-08-02
Topics:
Johnson, Alan T.
Wang, Liming
Gillett, Samuel J.
Chandraratna, Roshantha A. S.
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.
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