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ID: ALA3785043

Journal: Bioorg Med Chem Lett

Title: Exploring the purine core of 3'-C-ethynyladenosine (EAdo) in search of novel nucleoside therapeutics.

Authors: Hulpia F, Balzarini J, Schols D, Andrei G, Snoeck R, Van Calenbergh S.

Abstract: 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).

CiteXplore: 26965865

DOI: 10.1016/j.bmcl.2016.03.005