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.
MeSH terms
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Chemistry, Pharmaceutical / methods
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Crystallography, X-Ray
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Cyclobutanes / chemistry*
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Drug Design
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Humans
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Ligands
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Luciferases / metabolism
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Models, Chemical
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Molecular Conformation
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Phenyl Ethers / pharmacology
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Phenylacetates / pharmacology
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Protein Binding
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Structure-Activity Relationship
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Thyroid Gland / enzymology
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Thyroid Hormone Receptors alpha / metabolism
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Thyroid Hormone Receptors beta / chemistry*
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Thyroid Hormone Receptors beta / metabolism*
Substances
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3-cyclobutene-1,2-dione
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Cyclobutanes
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KB 141
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Ligands
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Phenyl Ethers
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Phenylacetates
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Thyroid Hormone Receptors alpha
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Thyroid Hormone Receptors beta
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Luciferases