A new class of high affinity thyromimetics containing a phenyl-naphthylene core.

Article Details

Citation
Copy to clipboard

Hangeland JJ, Friends TJ, Doweyko AM, Mellstrom K, Sandberg J, Grynfarb M, Ryono DE

A new class of high affinity thyromimetics containing a phenyl-naphthylene core.

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4579-84.

PubMed ID
16099653 [ View in PubMed
]
Abstract

High affinity thyromimetics containing a novel phenyl-naphthylene core are reported. The functionalized core is readily accessible via a Suzuki coupling protocol. Examples of this new class of TR ligands have sub-nanomolar binding affinities for the TRbeta receptor and low to modest selectivity for TRbeta. They also exhibit an SAR that diverges from other thyromimetics that are based on the diaryl ether core found in 3,5,3'-triiodothyronine.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
KB-141Thyroid hormone receptor alphaIC 50 (nM)25N/AN/ADetails
KB-141Thyroid hormone receptor betaIC 50 (nM)1.1N/AN/ADetails
LiothyronineThyroid hormone receptor alphaIC 50 (nM)0.24N/AN/ADetails
LiothyronineThyroid hormone receptor betaIC 50 (nM)0.26N/AN/ADetails