Synthesis and biological activity of retinoic acid receptor-alpha specific amides.

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Beard RL, Duong TT, Teng M, Klein ES, Standevan AM, Chandraratna RA

Synthesis and biological activity of retinoic acid receptor-alpha specific amides.

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3145-8.

PubMed ID
12372520 [ View in PubMed
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Abstract

Retinoids are analogues of all-trans-retinoic acid, a powerful hormone that mediates many fundamental biological processes. Cancer and other serious hyperproliferative diseases are attractive therapeutic targets for retinoids, but the therapeutic use of retinoids is limited due to severe toxicity. We report here the design of retinoid receptor-alpha specific ligands with growth inhibitory activity in breast cancer cell lines, and which do not cause the cutaneous toxicity associated with the currently available nonselective retinoid agonists.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
TretinoinRetinoic acid receptor alphaKd (nM)14N/AN/ADetails
TretinoinRetinoic acid receptor alphaEC 50 (nM)240N/AN/ADetails
TretinoinRetinoic acid receptor betaEC 50 (nM)38N/AN/ADetails
TretinoinRetinoic acid receptor betaKd (nM)11N/AN/ADetails
TretinoinRetinoic acid receptor gammaEC 50 (nM)6N/AN/ADetails
TretinoinRetinoic acid receptor gammaKd (nM)16N/AN/ADetails