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Issue 1, 2012
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Synthesis and in vitro enzymatic and antiviral evaluation of phosphoramidate d4T derivatives as chain terminators

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Abstract

The anti-HIV activity of nucleoside analogues is highly related to their substrate specificity for cellular and viral kinase and, as triphosphate, for HIV-RT. A series of phosphoramidate d4T derivatives have been synthesized and evaluated as substrates for HIV-1 RT, and also tested for their in vitro anti-HIV activity. Compounds 2 and 4 are able to inhibit HIV-1 replication to the same extent as d4T and d4TMP in MT-4 cells as well as in CEM/0 cells and CEM/TKcells. The data suggests that these phosphoramidates are hydrolysed to d4T before exerting their antiviral activity.

Graphical abstract: Synthesis and in vitro enzymatic and antiviral evaluation of phosphoramidate d4T derivatives as chain terminators

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Article information


Submitted
20 Jul 2011
Accepted
22 Sep 2011
First published
08 Nov 2011

Org. Biomol. Chem., 2012,10, 146-153
Article type
Paper

Synthesis and in vitro enzymatic and antiviral evaluation of phosphoramidate d4T derivatives as chain terminators

S. Yang, C. Pannecouque, E. Lescrinier, A. Giraut and P. Herdewijn, Org. Biomol. Chem., 2012, 10, 146
DOI: 10.1039/C1OB06214J

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