Peyrottes S, Gosselin G, Aubertin A M, Périgaud C
Laboratoire de Chimie Organique Biomoléculaire de Synthèse, Université Montpellier II, UMR 5625 CNRS, Montpellier, France.
Nucleosides Nucleotides Nucleic Acids. 2003 May-Aug;22(5-8):903-5. doi: 10.1081/NCN-120022682.
Synthesis and biological activities of several phosphotriester derivatives of 3'-azido-2',3'-dideoxythymidine (AZT) bearing a S-pivaloyl-2-thioethyl (tBuSATE) group and aryl residues derived from L-tyrosine are reported. All compounds showed marked anti-HIV activity in thymidine kinase-deficient CEM cells demonstrating their ability to deliver intracellularly the parent 5'-mononucleotide.
报道了几种3'-叠氮基-2',3'-双脱氧胸苷（AZT）的磷酸三酯衍生物的合成及其生物活性，这些衍生物带有S-新戊酰基-2-硫代乙基（tBuSATE）基团以及源自L-酪氨酸的芳基残基。所有化合物在缺乏胸苷激酶的CEM细胞中均表现出显著的抗HIV活性，证明了它们在细胞内递送母体5'-单核苷酸的能力。
