Prostaglandin E₂ (PGE₂) is a lipid mediator of inflammation and its inhibition has become a popular drug target due to its harmful physiological roles. Diarylheptanoids are one class of compounds that have shown successful inhibition of PGE₂. This paper reports the synthesis and PGE₂ inhibitory activity of a series of analogues of a naturally occurring diarylheptanoid. The most efficacious compounds were examined for dose-dependent PGE₂ inhibition. Among several promising compounds, the lead candidate exhibited an IC₅₀ value of 0.56 ng/µL or 1.7 µM with no detectable toxicity at the highest dose of 10 ng/µL.

中文翻译：

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新型二芳基庚烷的合成及PGE ₂抑制活性

前列腺素E ₂（PGE ₂）是炎症的脂质介质，由于其有害的生理作用，其抑制作用已成为流行的药物靶标。二芳基庚烷类化合物是已显示出成功抑制PGE _2的一类化合物。本文报道了一系列天然存在的二芳基庚烷类似物的合成和PGE ₂抑制活性。检查了最有效的化合物对剂量依赖性PGE _2的抑制作用。在几种有前途的化合物中，潜在候选化合物的IC ₅₀值为0.56 ng / µL或1.7 µM，在最高剂量为10 ng / µL时没有可检测到的毒性。