Agback, Peter
- Karo Bio AB
Abstract
Based on the recently described concept of "indirect antagonism" of nuclear receptors, a series of thyroid hormone receptor (TR) antagonists were prepared, in which the outer ring of a thyromimetic was replaced with alkyl chains of variable length and branch. The results of a binding assay for the human TR and reporter cell assay revealed, within this series, a positive correlation between increasing bulk of the alkyl group and affinity to TRs. Compared with already reported TR antagonists, their affinities are within the same range, thus potentially representing a useful approach to novel and high affinity TR-antagonists.
Published in
Journal of Medicinal Chemistry
2005, volume: 48, number: 9, pages: 3114-3117
Publisher: AMER CHEMICAL SOC
SLU Authors
UKÄ Subject classification
Organic Chemistry
Publication identifier
- DOI: https://doi.org/10.1021/jm050004k
Permanent link to this page (URI)
https://res.slu.se/id/publ/83905