双吗啉及其碳环核苷的合成与生物活性
Synthesis and biological activity of bimorpholine and its carbanucleoside.
作者信息
Ausmees Kerti, Selyutina Anastasia, Kütt Kristel, Lippur Kristin, Pehk Tõnis, Lopp Margus, Zusinaite Eva, Merits Andres, Kanger Tõnis
机构信息
Department of Chemistry, Tallinn University of Technology, Tallinn, Estonia.
出版信息
Nucleosides Nucleotides Nucleic Acids. 2011 Nov;30(11):897-907. doi: 10.1080/15257770.2011.621919.
A new enantiomerically pure carbacyclic nucleoside analogue with bimorpholine as a nonaromatic nucleobase was synthesized. The nucleoside analogue and bimorpholine were tested for cytotoxicity using an MTT assay and the xCELLigence System. Both assays revealed that compound 3 was highly cytotoxic at a 50 μM concentration while the cytotoxic effect of compound 1 was much less prominent. No antiretroviral activity was detected for this compound. In contrast, it acted as a potent inhibitor of hepatitis C virus (HCV) replication. Most likely this effect originates largely from the cytotoxicity of the compound; however, it is possible that a specific mechanism of HCV inhibition also exists.
合成了一种新的对映体纯的碳环核苷类似物，其非芳香族核碱基为双吗啉。使用MTT法和xCELLigence系统对该核苷类似物和双吗啉进行了细胞毒性测试。两种测定均显示，化合物3在50 μM浓度时具有高细胞毒性，而化合物1的细胞毒性作用则不那么显著。未检测到该化合物的抗逆转录病毒活性。相反，它是丙型肝炎病毒（HCV）复制的有效抑制剂。很可能这种作用主要源于该化合物的细胞毒性；然而，也有可能存在特定的HCV抑制机制。
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