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Synthesis and antiviral evaluation of α-L-2'-deoxythreofuranosyl nucleosides.

Abstract：

:The synthesis of a series of α-L-2'-deoxythreofuranosyl nucleosides featuring the nucleobases A, T, C and U is described in seven steps from 1,2-O-isopropyledene-α-L-threose, involving a Vorbrüggen coupling and a Barton-McCombie deoxygenation protocol as the key steps. All analogues, including a phosphoramidate nucleoside phosphate prodrug of the T analogue, were evaluated against a broad panel of different viruses but found inactive, while also lacking notable cellular toxicity. The thymidine analogue showed inhibition to mitochondrial thymidine kinase-2 (TK-2), herpes simplex virus type 1 (HSV-1) TK, varicella-zoster virus (VZV) TK and Mycobacterium tuberculosis thymidylate kinase.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Toti KS,Derudas M,McGuigan C,Balzarini J,Van Calenbergh S

doi

10.1016/j.ejmech.2011.05.036

subject

Has Abstract

pub_date

2011-09-01 00:00:00

pages

3704-13

issue

9

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(11)00416-8

journal_volume

46

pub_type

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