新型季铵盐莰烷衍生物及其抗病毒活性、遗传毒性和细胞毒性。
New quaternary ammonium camphor derivatives and their antiviral activity, genotoxic effects and cytotoxicity.
机构信息
N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch, Russian Academy of Sciences, Lavrentjev Avenue 9, 630090 Novosibirsk, Russia; Novosibirsk State University, Pirogova St. 2, 630090 Novosibirsk, Russia.
出版信息
Bioorg Med Chem. 2013 Nov 1;21(21):6690-8. doi: 10.1016/j.bmc.2013.08.014. Epub 2013 Aug 12.
The synthesis and biological evaluation of a novel series of dimeric camphor derivatives are described. The resulting compounds were studied for their antiviral activity, cyto- and genotoxicity. Compounds 3a and 3d in which the quaternary nitrogen atoms are separated by the C5H10 and С9H18 aliphatic chain, exhibited the highest efficiency as an agent inhibiting the reproduction of the influenza virus A(H1N1)pdm09. The cytotoxicity data of compounds 3 and 4 revealed their moderate activity against malignant cell lines; compound 3f had the highest activity for the CEM-13 cells. These results show close agreement with the data of independent studies on toxicity of these compounds, in particular that the toxicity of compounds strongly depends on spacer length.
描述了一系列新型二聚莰烷衍生物的合成和生物评价。研究了所得化合物的抗病毒活性、细胞毒性和遗传毒性。其中化合物 3a 和 3d 中，季氮原子通过 C5H10 和 С9H18 脂肪链隔开，表现出最高的抑制甲型流感病毒 A(H1N1)pdm09 复制的效率。化合物 3 和 4 的细胞毒性数据表明它们对恶性细胞系具有中等活性；化合物 3f 对 CEM-13 细胞的活性最高。这些结果与这些化合物毒性的独立研究数据非常吻合，特别是化合物的毒性强烈依赖于间隔物的长度。
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