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

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 ?M, respectively). Derivative 10 on the other hand was found active against varicella zoster virus (EC50: 4.68 ?M).

SUBMITTER: Hulpia F

PROVIDER: S-EPMC7126545 | biostudies-literature | 2016 Apr

REPOSITORIES: biostudies-literature

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

Hulpia Fabian F Balzarini Jan J Schols Dominique D Andrei Graciela G Snoeck Robert R Van Calenbergh Serge S

Bioorganic & medicinal chemistry letters 20160303 8

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 ...[more]

PMID: 26965865

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