188887-76-5Relevant articles and documents
SYNTHESIS AND USE OF RETINOID COMPOUNDS HAVING NEGATIVE HORMONE AND/OR ANTAGONIST ACTIVITIES
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, (2008/06/13)
2,2-Dialkyl-4-aryl-substituted benzopyran and benzothiopyran derivatives of the formula STR1 where the symbols have the meaning described in the specification, have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists.
High affinity retinoic acid receptor antagonists: Analogs of AGN 193109
Johnson, Alan T.,Wang, Liming,Gillett, Samuel J.,Chandraratna, Roshantha A. S.
, p. 573 - 576 (2007/10/03)
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.