Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands.

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Raval S, Raval P, Bandyopadhyay D, Soni K, Yevale D, Jogiya D, Modi H, Joharapurkar A, Gandhi N, Jain MR, Patel PR

Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):3919-24. doi: 10.1016/j.bmcl.2008.06.038. Epub 2008 Jun 14.

PubMed ID
18585912 [ View in PubMed
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Abstract

Design and synthesis of a novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives are reported and their in vitro thyroid hormone receptor selectivity has been evaluated in the thyroid luciferase receptor assay. The 3-[3,5-dichloro-4-(4-hydroxy-3-isopropylphenoxy)-phenylamino]-4-hydroxy-cyclobut- 3-ene-1,2-dione 21 has shown selectivity towards thyroid hormone receptor beta.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
KB-141Thyroid hormone receptor alphaEC 50 (nM)4.5N/AN/ADetails
KB-141Thyroid hormone receptor betaEC 50 (nM)1.12N/AN/ADetails