Syntheses and evaluation of naphthalenyl- and chromenyl-pyrrolyl-benzoic acids as potent and selective retinoic acid receptor alpha agonists.
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Hibi S, Tagami K, Kikuchi K, Yoshimura H, Tai K, Hida T, Tokuhara N, Yamauchi T, Nagai M
Syntheses and evaluation of naphthalenyl- and chromenyl-pyrrolyl-benzoic acids as potent and selective retinoic acid receptor alpha agonists.
Bioorg Med Chem Lett. 2000 Apr 3;10(7):623-5.
- PubMed ID
- 10762039 [ View in PubMed]
- Abstract
Synthesis and structure activity relationships (SAR) of RAR alpha-selective agonists are discussed. 4-[5-(5,8-Dimethyl-2H-3-chromenyl)-1H-2-pyrrolyl]benzoic acid (12a), which possesses a flat structural moiety and an oxygen atom at the hydrophobic part, showed highly selective transactivation activity at the RAR alpha receptor.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Tretinoin Retinoic acid receptor alpha IC 50 (nM) 0.89 N/A N/A Details Tretinoin Retinoic acid receptor beta IC 50 (nM) 0.94 N/A N/A Details Tretinoin Retinoic acid receptor gamma IC 50 (nM) 0.62 N/A N/A Details