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Inhibition of Cytokine Production by Hymenialdisine Derivatives

机译:菊苣碱衍生物对细胞因子产生的抑制作用

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摘要

We describe herein the synthesis and biological activity of two indoloazepines that are structurally related to the marine sponge metabolite hymenialdisine. The natural product hymenialdisine was found to be a potent inhibitor of interleukin-2 (IC_(50) = 2.4 μM) and tumor necrosis factor α (IC_(50) = 1.4 μM) production. One of the hymenialdisine derived indoloazepines was found to also inhibit interleukin-2 (IC_(50) = 3.5 μM) and tumor necrosis factor α (IC_(50) = 8.2 μM) production.
机译:我们在本文中描述了两个与海洋海绵代谢产物猴头二素在结构上相关的吲哚并氮杂的合成和生物活性。发现天然产物土生虫草苷是白细胞介素2(IC_(50)= 2.4μM)和肿瘤坏死因子α(IC_(50)= 1.4μM)产生的有效抑制剂。发现一种从菊苣二碱衍生的吲哚并西平也抑制白介素2(IC_(50)= 3.5μM)和肿瘤坏死因子α(IC_(50)= 8.2μM)的产生。

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