Bioorganic and Medicinal Chemistry Letters p. 2865 - 2870 (1996)
Update date:2022-08-12
Topics:
Yu, Kuo-Long
Ostrowski, Jacek
Chen, Simon
Tramposch, Kenneth M.
Reczek, Peter R.
Mansuri, Muzammil M.
Starrett Jr., John E.
The keto linker of 2-naphthoate retinoid 1 has been found nonessential for RAR transactivation activity and can be replaced with heteroatoms such as S, O, N without significant reduction of the activity. On the other hand, substitutions on the aromatic rings of retinoids 1 and 2 resulted in analogs with reduced potentcy and RAR selectivity.
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