ChemInform Abstract: Synthesis and Biological Activity of Novel Thyroid Hormone Analogues: 5′-Aryl Substituted GC-1 Derivatives.
Abstract
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ChemInform Abstract
Eleven 5′-substituted GC-1 analogues like (VIII) and (XII) are synthesized to explore the effect of GC-1 core structure modifications on binding to thyroid hormone receptor isoforms and activation of transcription. This approach is based on ortho lithiation and in-situ boration of the biarylmethane (I), a key intermediate of the revised GC-1 synthesis, followed by Suzuki cross-coupling. All of the new compounds show reduced binding affinity, but most of the compounds retain TRβ-selectivity. All compounds are nearly full agonists of TRβ activation, except (VIIIb), which antagonizes the response to thyroid hormone.
