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4-[3-(5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)phenyl]benzoic Acid and Heterocyclic-Bridged Analogues Are Novel Retinoic Acid Receptor Subtype and Retinoid X Receptor Alpha Agonists

M I Dawson, L Jong, P D Hobbs, D Xiao, K C Feng, W R Chao, C Pan, J A Fontana, X K Zhang

Bioorg Med Chem Lett. 2000 Jun 19;10(12):1311-3.

PMID: 10890153

Abstract:

Aromatic retinoids having a meta-substituted aromatic ring bridge, such as 4-[3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)phenyl]benzo ic acid and its 3,5-diaryl-substituted 4,5-dihydroisoxazole analogue, function as retinoid receptor panagonists by activating both retinoic acid and retinoid X receptors to induce gene transcription, and thereby provide novel scaffolds for retinoid drug development. Both classes of these ligand-inducible transcription factors are involved in mediating the inhibitory effects of retinoids on cancer cell growth.

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