Synthesis and in vitro enzymatic and antiviral evaluation of phosphoramidate d4T derivatives as chain terminators,10.1039/C1OB06214J

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

Shiqiong Yang,Christophe Pannecouque,Eveline Lescrinier,Anne Giraut,Piet Herdewijn

Organic & Biomolecular Chemistry Pub Date : 11/08/2011 00:00:00 , DOI:10.1039/C1OB06214J

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/TK⁻cells. The data suggests that these phosphoramidates are hydrolysed to d4T before exerting their antiviral activity.