Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 50, Issue 22, Pages 5269-5280Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm070556y
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Funding
- NIDDK NIH HHS [R01 DK058080-05, R01 DK58080, R01 DK058080, R55 DK058080, R01 DK058080-06] Funding Source: Medline
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The modulation of gene regulation by blocking the interaction between the thyroid receptor (TR) and obligate coregulators has been reported recently with the discovery of the lead compound 3-(dimethylamino)-1-(4-hexylphenyl)propan-1-one). Herein we report studies aimed at optimization of this initial hit to determine the basic parameters of the structure -activity relationships and clarify the mechanism of action. These studies provided new insights, showing that activity and TR beta isoform selectivity is highly correlated with the structural composition of these covalent inhibitors.
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