Novel heterocyclic thyromimetics.
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.
Haning
Helmut
H
BAYER HealthCare AG, Business Group Pharma, D-42096 Wuppertal, Germany. helmut.haning@bayerhealthcare.com
Woltering
Michael
M
Mueller
Ulrich
U
Schmidt
Gunter
G
Schmeck
Carsten
C
Voehringer
Verena
V
Kretschmer
Axel
A
Pernerstorfer
Josef
J
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
D006571:Heterocyclic Compounds; D007191:Indazoles; D007211:Indoles; D008024:Ligands; D010636:Phenols; D011988:Receptors, Thyroid Hormone; D014284:Triiodothyronine