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
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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
DrugTargetPropertyMeasurementpHTemperature (°C)
TretinoinRetinoic acid receptor alphaIC 50 (nM)0.89N/AN/ADetails
TretinoinRetinoic acid receptor betaIC 50 (nM)0.94N/AN/ADetails
TretinoinRetinoic acid receptor gammaIC 50 (nM)0.62N/AN/ADetails