Novel heterocyclic thyromimetics

…, V Voehringer, A Kretschmer, J Pernerstorfer

Index: Haning, Helmut; Woltering, Michael; Mueller, Ulrich; Schmidt, Gunter; Schmeck, Carsten; Voehringer, Verena; Kretschmer, Axel; Pernerstorfer, Josef Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 7 p. 1835 - 1840

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Citation Number: 21

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