Author: Hulpia, Fabian; Balzarini, Jan; Schols, Dominique; Andrei, Graciela; Snoeck, Robert; Van Calenbergh, Serge
Title: Exploring the purine core of 3′-C-ethynyladenosine (EAdo) in search of novel nucleoside therapeutics Cord-id: oshmehqb Document date: 2016_4_15
ID: oshmehqb
Snippet: 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 (EC(50): 0.31 and 51 μM, respectively). Derivative 10 on the other hand was
Document: 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 (EC(50): 0.31 and 51 μM, respectively). Derivative 10 on the other hand was found active against varicella zoster virus (EC(50): 4.68 μM).
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