| Literature DB >> 8691435 |
K L Yu1, P Spinazze, J Ostrowski, S J Currier, E J Pack, L Hammer, T Roalsvig, J A Honeyman, D R Tortolani, P R Reczek, M M Mansuri, J E Starrett.
Abstract
In search for retinoic acid receptor (RAR) selective ligands, a series of 6-substituted 2-naphthoic acid retinoids were synthesized and evaluated in vitro in a transactivation assay and a competition binding assay for all RARs. These derivatives, in general, showed RAR beta,gamma selectivity. Among these naphthoic acids, oxime derivative 12 was identified as a potent RAR gamma-selective retinoid, while olefinic derivative 11 was found to be comparable to retinoic acid and slightly RAR beta,gamma selective. For the bioassays, a general correlation was observed between the binding affinity of the ligand to the receptors and the potency of the compounds in the transactivation assay. The structure-activity relationship of these naphthoic acids will be discussed.Entities:
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Year: 1996 PMID： 8691435 DOI： 10.1021/jm9502293
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446