High affinity retinoic acid receptor antagonists: Analogs of AGN 193109

DOI: 10.1016/S0960-894X(99)00047-5

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 573 - 576 (1999)

Update date:2022-08-02

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Authors:

Johnson, Alan T.

Wang, Liming

Gillett, Samuel J.

Chandraratna, Roshantha A. S.

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Article abstract of DOI:10.1016/S0960-894X(99)00047-5

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.

Full text of DOI:10.1016/S0960-894X(99)00047-5

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