Novel heterocyclic thyromimetics.

Helmut Haning; Michael Woltering; Ulrich Mueller; Gunter Schmidt; Carsten Schmeck; Verena Voehringer; Axel Kretschmer; Josef Pernerstorfer

doi:10.1016/j.bmcl.2005.02.028

PubMed · 15780617

Novel heterocyclic thyromimetics.

Helmut Haning·Michael Woltering·Ulrich Mueller·Gunter Schmidt·Carsten Schmeck·Verena Voehringer·Axel Kretschmer·Josef Pernerstorfer

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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.

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Animals Binding Sites Biological Assay Heterocyclic Compounds Indazoles Indoles Ligands Molecular Mimicry Phenols Receptors, Thyroid Hormone Structure-Activity Relationship Transfection Triiodothyronine Journal Article

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Helmut Haning, Michael Woltering, Ulrich Mueller, Gunter Schmidt, Carsten Schmeck, Verena Voehringer, Axel Kretschmer, Josef Pernerstorfer. 2005-04-01. Novel heterocyclic thyromimetics.. https://doi.org/10.1016/j.bmcl.2005.02.028

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