Abstract
Novel heterocycle-fused thyromimetics are presented carrying indoles or indazoles instead of the phenolic group in T3. Potent agonists were identified in both series. SAR trends are examined and found to be mostly consistent with previously published thyromimetics. Moderate THRbeta selectivity (approx. 10-fold) was observed in the indole series using isoform-selective transient THR transfection assays.
MeSH terms
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Animals
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Binding Sites
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Biological Assay
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Heterocyclic Compounds / chemical synthesis*
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Heterocyclic Compounds / pharmacology
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Indazoles / chemistry
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Indoles / chemistry
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Ligands
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Molecular Mimicry*
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Phenols / chemistry
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Receptors, Thyroid Hormone / agonists*
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Structure-Activity Relationship
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Transfection
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Triiodothyronine / pharmacology
Substances
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Heterocyclic Compounds
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Indazoles
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Indoles
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Ligands
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Phenols
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Receptors, Thyroid Hormone
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Triiodothyronine