Abstract
A new high-affinity thyroid hormone antagonist 6 with druglike properties was designed and synthesized. The compound behaved as an antagonist in a cell transactivation assay, and in a first in vivo experiment in rats.
MeSH terms
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Animals
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CHO Cells
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Cricetinae
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Cricetulus
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Humans
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Ligands
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Models, Molecular
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Phenylpropionates / chemical synthesis*
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Phenylpropionates / chemistry
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Phenylpropionates / pharmacology
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / pharmacology
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Rats
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Receptors, Thyroid Hormone / antagonists & inhibitors*
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Thyroid Hormone Receptors alpha / antagonists & inhibitors
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Thyroid Hormone Receptors beta / antagonists & inhibitors
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Thyroid Hormone Receptors beta / chemistry
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Transcriptional Activation / drug effects
Substances
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3-(3,5-dibromo-4-(4-hydroxy-3-isopropyl-5-(2-pyridin-4-ylvinyl)phenoxy)phenyl)propionic acid
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Ligands
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Phenylpropionates
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Pyridines
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Receptors, Thyroid Hormone
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Thyroid Hormone Receptors alpha
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Thyroid Hormone Receptors beta