Novel retinoic acid receptor alpha agonists: syntheses and evaluation of pyrazole derivatives.

Article Details

Citation
Copy to clipboard

Kikuchi K, Hibi S, Yoshimura H, Tai K, Hida T, Tokuhara N, Yamauchi T, Nagai M

Novel retinoic acid receptor alpha agonists: syntheses and evaluation of pyrazole derivatives.

Bioorg Med Chem Lett. 2000 Apr 3;10(7):619-22.

PubMed ID
10762038 [ View in PubMed
]
Abstract

We have designed and synthesized a series of pyrazole derivatives as candidate retinoic acid receptor (RAR) agonists. One of them, 4-[5-(1, 5-diisopropyl-1H-3-pyrazolyl)-1H-2-pyrrolyl]benzoic acid (11b), which possesses a 2,5-disubstituted pyrrole moiety, showed selective transactivation activity for the RAR alpha receptor, and had highly potent cell-differentiating activity on HL-60 cells.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
TretinoinRetinoic acid receptor alphaIC 50 (nM)0.78N/AN/ADetails
TretinoinRetinoic acid receptor betaIC 50 (nM)0.9N/AN/ADetails
TretinoinRetinoic acid receptor gammaIC 50 (nM)0.5N/AN/ADetails