Design, synthesis, biological evaluation and docking studies of pterostilbene analogs inside PPARalpha.

Mizuno CS; Ma G; Khan SPatny AAvery MARimando AM

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Design, synthesis, biological evaluation and docking studies of pterostilbene analogs inside PPARalpha.

机译：Design, synthesis, biological evaluation and docking studies of pterostilbene analogs inside PPARalpha.

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摘要

Pterostilbene, a naturally occurring analog of resveratrol, has previously shown PPARalpha activation in H4IIEC3 cells and was found to decrease cholesterol levels in animals. In this study, analogs of pterostilbene were synthesized and their ability to activate PPARalpha was investigated. Among analogs that was synthesized (E)-4-(3,5-dimethoxystyryl)phenyl dihydrogen phosphate showed activity higher than pterostilbene and control drug ciprofibrate. Docking of the stilbenes inside PPARalpha showed the presence of important hydrogen bond interactions for PPARalpha activation.

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《Bioorganic and medicinal chemistry》 |2008年第7期|3800-3808|共9页
作者
Mizuno CS; Ma G; Khan SPatny AAvery MARimando AM;
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作者单位

USDA-ARS, Natural Products Utilization Research Unit, PO Box 8048, University, MS 38677, United States.;

ost.saga-med.ac.jp;

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正文语种英语
中图分类药学;生物化学;
关键词
Animals; Cell Line; Tumor; Drug Design; Ligands; Models; Molecular; Molecular Structure; 动物; 药物设计; 配体; 模型; 分子; 分子结构; 蛋白质结合; 大鼠; 芪类;

Design, synthesis, biological evaluation and docking studies of pterostilbene analogs inside PPARalpha.

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