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Sammanfattning

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.

Publicerad i

Journal of Medicinal Chemistry
2005, volym: 48, nummer: 9, sidor: 3114-3117
Utgivare: AMER CHEMICAL SOC

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Organisk kemi

Publikationens identifierare

  • DOI: https://doi.org/10.1021/jm050004k

Permanent länk till denna sida (URI)

https://res.slu.se/id/publ/83905