A designed antagonist of the thyroid hormone receptor

Bioorganic & Medicinal Chemistry Letters
2001.0

Abstract

We synthesized an analogue of the thyromimetic GC-1 bearing the same hydrophobic appendage as the estrogen receptor antagonist ICI-164,384. While having reduced affinity for the thyroid hormone receptors compared to GC-1, it behaves in a manner consistent with a competitive antagonist in a transactivation assay.

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