Novel heterocyclic thyromimetics

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• 作者：Haning ; Helmut ; Woltering ; Michael ; Mueller ; Ulrich ; Schmidt ; Gunter ; Schmeck ; Carsten ; Voehringer ; Verena ; et. al.
• 关键词：Thyromimetics ; Indoles ; Indazoles
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2005
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：April 1, 2005
• 卷：15
• 期：7
• 页码：1835-1840
• 文件大小：130 K

摘要

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 THR脦脦 selectivity (approx. 10-fold) was observed in the indole series using isoform-selective transient THR transfection assays