期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 50, 期 22, 页码 5269-5280出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm070556y
关键词
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资金
- NIDDK NIH HHS [R01 DK058080-05, R01 DK58080, R01 DK058080, R55 DK058080, R01 DK058080-06] Funding Source: Medline
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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