Exploring the purine core of 3‿C-ethynyladenosine (EAdo) in search of novel nucleoside therapeutics

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• 作者：Fabian Hulpia^a ; Jan Balzarini^b ; Dominique Schols^b ; Graciela Andrei^b ; Robert Snoeck^b ; Serge Van Calenbergh^a ; ^{Serge.VanCalenbergh@ugent.be" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Nucleosides ; 3&prime ; -C-Ethynyladenosine ; Vorbrü ; ggen coupling
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 April 2016
• 年：2016
• 卷：26
• 期：8
• 页码：1970-1972
• 全文大小：361 K

文摘

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).