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Updated: Jul 15, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Novel heterocyclic thyromimetics. Part 2
Helmut Haning1, Ulrich Mueller, Gunter Schmidt
1Bayer HealthCare AG, Bayer Schering Pharma Global Drug Discovery, D-42096 Wuppertal, Germany. Helmut.Haning@bayerhealthcare.com
Abstract:
Novel heterocyclic thyromimetics are presented carrying carboxy-substituted benzofurans or sulfur containing heterocycles, as replacements for the amino acid side chain of T3. Potent agonists were identified in both series. SAR trends are examined and found to be mostly consistent with previously published thyromimetics. The lack of isoform selectivity demonstrated with isoform-selective transient THR transfection assays has been confirmed by corresponding in vivo studies.
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