探索3'-C-乙炔基腺苷（EAdo）的嘌呤核心以寻找新型核苷疗法。
Exploring the purine core of 3'-C-ethynyladenosine (EAdo) in search of novel nucleoside therapeutics.
作者信息
Hulpia Fabian, Balzarini Jan, Schols Dominique, Andrei Graciela, Snoeck Robert, Van Calenbergh Serge
机构信息
Laboratory for Medicinal Chemistry, Ghent University, Ottergemsesteenweg 460, B-9000 Ghent, Belgium.
KU Leuven, Rega Institute for Medical Research, Minderbroedersstraat 10, B-3000 Leuven, Belgium.
出版信息
Bioorg Med Chem Lett. 2016 Apr 15;26(8):1970-2. doi: 10.1016/j.bmcl.2016.03.005. Epub 2016 Mar 3.
A series of new nucleoside analogues based on a C-3 branched ethynyl sugar derivative as present in 3'-C-ethynylcytidine (ECyd) and -adenosine (EAdo), combined with modified purine bases was synthetized and evaluated against a broad array of viruses and tumour cell lines. The pronounced cytostatic activity of EAdo was confirmed. EAdo and its 2,6-diaminopurine analogue showed inhibitory activity against vaccinia virus (EC50: 0.31 and 51 μM, respectively). Derivative 10 on the other hand was found active against varicella zoster virus (EC50: 4.68 μM).
合成了一系列基于3'-C-乙炔基胞苷（ECyd）和-腺苷（EAdo）中存在的C-3支链乙炔基糖衍生物，并结合修饰嘌呤碱基的新型核苷类似物，并针对多种病毒和肿瘤细胞系进行了评估。证实了EAdo具有显著的细胞生长抑制活性。EAdo及其2,6-二氨基嘌呤类似物对痘苗病毒表现出抑制活性（EC50分别为0.31和51 μM）。另一方面，衍生物10被发现对水痘带状疱疹病毒有活性（EC50：4.68 μM）。
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