title: Novel heterocyclic thyromimetics.
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 THRbeta selectivity (approx. 10-fold) was observed in the indole series using isoform-selective transient THR transfection assays.
authors.affiliation: BAYER HealthCare AG, Business Group Pharma, D-42096 Wuppertal, Germany. helmut.haning@bayerhealthcare.com
authors.forename: Helmut
authors.initials: H
authors.lastname: Haning
authors.forename: Michael
authors.initials: M
authors.lastname: Woltering
authors.forename: Ulrich
authors.initials: U
authors.lastname: Mueller
authors.forename: Gunter
authors.initials: G
authors.lastname: Schmidt
authors.forename: Carsten
authors.initials: C
authors.lastname: Schmeck
authors.forename: Verena
authors.initials: V
authors.lastname: Voehringer
authors.forename: Axel
authors.initials: A
authors.lastname: Kretschmer
authors.forename: Josef
authors.initials: J
authors.lastname: Pernerstorfer
mesh_terms: D000818:Animals; D001665:Binding Sites; D001681:Biological Assay; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D007191:Indazoles / Q000737:chemistry; D007211:Indoles / Q000737:chemistry; D008024:Ligands; D018716:Molecular Mimicry; D010636:Phenols / Q000737:chemistry; D011988:Receptors, Thyroid Hormone / Q000819:agonists*; D013329:Structure-Activity Relationship; D014162:Transfection; D014284:Triiodothyronine / Q000494:pharmacology
chemical_list: D006571:Heterocyclic Compounds; D007191:Indazoles; D007211:Indoles; D008024:Ligands; D010636:Phenols; D011988:Receptors, Thyroid Hormone; D014284:Triiodothyronine