6'-氟-3-去氮杂氮胞苷：合成及其抗病毒特性，包括对埃博拉病毒的作用
6'-Fluoro-3-deazaneplanocin: Synthesis and antiviral properties, including Ebola.
作者信息
Liu Chong, Chen Qi, Cardinale Steven, Bowlin Terry L, Schneller Stewart W
机构信息
Molette Laboratory for Drug Discovery, Department of Chemistry and Biochemistry, Auburn University, Auburn, AL 36849-5312, United States.
Department of Chemistry, Slippery Rock University, Slippery Rock, PA 16057, United States.
出版信息
Bioorg Med Chem Lett. 2018 Dec 15;28(23-24):3674-3675. doi: 10.1016/j.bmcl.2018.10.030. Epub 2018 Oct 22.
A convenient stereospecific synthesis of 6'-fluoro-3-deazaneplanocin (6) has been accomplished from d-ribose in 15 steps. It is reported to possess significant activity towards Ebola (Zaire, Vero, μM: EC < 0.36; CC 125; SI > 347) with moderate inhibition of the target enzyme (S-adenosylhomocysteine hydrolase), which did not correlate directly with its anti-Ebola effects. Compound 6, with limited cytotoxicity, also displayed activity against measles, H1N1 and Pichinde.
已从d-核糖出发，通过15步反应方便地立体定向合成了6'-氟-3-脱氮甲苷（6）。据报道，它对埃博拉病毒（扎伊尔型、Vero细胞，微摩尔：EC＜0.36；CC 125；SI＞347）具有显著活性，对靶酶（S-腺苷同型半胱氨酸水解酶）有中度抑制作用，但其抗埃博拉作用与之并无直接关联。化合物6具有有限的细胞毒性，还对麻疹、H1N1和皮钦德病毒显示出活性。
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