Jia, Xiao; Weber, Stefan; Schols, Dominique; Meier, Chris published the artcile< Membrane Permeable, Bioreversibly Modified Prodrugs of Nucleoside Diphosphate-γ-Phosphonates>, Application In Synthesis of 112-63-0, the main research area is DNA polymerase antiviral antitumor nucleotide preparation; antiviral anticancer phosphorylation metabolite phosphonate nucleoside HIV human; prodrug nucleoside phosphate phosphonate transcriptase inhibitor.
Nucleoside reverse transcriptase inhibitors (NRTIs) are widely used as antiviral and anticancer agents although they require intracellular phosphorylation into their antiviral active form, the triphosphorylated nucleoside analog metabolites. We report on the synthesis and characterization of a new class of nucleoside triphosphate analogs comprising a C-alkyl-phosphonate moiety replacing the γ-phosphate. These compounds were converted into bio-reversible modified lipophilic prodrugs at the γ-phosphonate by γ-C-(alkyl)-nucleoside triphosphate analogs with high selectivity due to an enzyme-triggered delivery mechanism. The later compounds were very stable in CEM cell extracts and they were substrates for HIV-RT without being substrates for DNA-polymerases α, β and γ. In antiviral assays, excellent antiviral activity of the prodrugs was found in CEM/0 cells was completely kept in CEM/TK- cells. The activity was improved by 3 logs as compared to the parent nucleoside d4T.
Journal of Medicinal Chemistry published new progress about AIDS (disease). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application In Synthesis of 112-63-0.
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