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首页> 外文期刊>Bulletin of the Korean Chemical Society >The Cytotoxic Activity of Honokiol‐Triazole Derivatives in Ovarian Cancer Cells
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The Cytotoxic Activity of Honokiol‐Triazole Derivatives in Ovarian Cancer Cells

机译:卵巢癌细胞中HOPIOL-三唑衍生物的细胞毒性活性

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Honokiol‐triazole derivatives (4–17) were synthesized via click reactions between 2‐ or 4′‐propargylated honokiol and azide compounds. Their anticancer activities were evaluated by using two ovarian cancer cells (A2780 and OVCAR3). Among the 14 compounds, compound 5 coupled with 4′‐propargylated honokiol and benzyl azide exhibited relatively potent cytotoxic activity (IC50?=?5.5?±?0.5?μM for A2780 and IC50?=?3.97?±?0.6?μM for OVCAR3) but was less toxic to normal cells (IC50?=?18.90?±?0.9?μM for IOSE80PC). The cytotoxic effect of compound 5 is associated with caspase‐dependent apoptotic cell death via induction of intracellular reactive oxygen species.
机译:通过咔哒反应合成HONOKIOL-三唑衍生物(4-17),在2-或4'-丙基丙基醇和叠氮化合物之间的反应合成。通过使用两种卵巢癌细胞(A2780和OVCAR3)来评估它们的抗癌活动。在14个化合物中,与4'-丙基丙基醇和苄乙氧化物偶联的化合物5表现出相对有效的细胞毒性活性(IC50?=Δ5.5?±5.5?±5.5?μm,用于A2780和IC50?=Δ3.97?±0.6?μm为OVCAR3 )但对正常细胞毒性较小(IC50?= 18.90?±0.9?μm)。化合物5的细胞毒性效应通过诱导细胞内反应性氧物质与依赖胱天蛋白酶依赖性凋亡细胞死亡有关。

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