抗HIV前体核苷酸：分解途径及其与生物活性的相关性
Anti-HIV pronucleotides: decomposition pathways and correlation with biological activities.
作者信息
Egron D, Lefebvre I, Périgaud C, Beltran T, Pompon A, Gosselin G, Aubertin A M, Imbach J L
机构信息
Laboratoire de Chimie Bioorganique, UMR CNRS-USTL 5625, Université Montpellier II, France.
出版信息
Bioorg Med Chem Lett. 1998 May 5;8(9):1045-50. doi: 10.1016/s0960-894x(98)00158-9.
The purpose of the present study was to compare the decomposition pathways in CEM cell extracts of various phenyl phosphoramidate derivatives of AZT. In addition, the structures of their metabolites were identified. Correlations with their anti-HIV activities in a thymidine kinase deficient (TK-) CEM cell line have been established with a rationale of designing phosphoramidate pronucleotides capable of delivering intracellularly their respective 5'-nucleoside monophosphate derivatives.
本研究的目的是比较齐多夫定（AZT）的各种苯基磷酰胺酯衍生物在CEM细胞提取物中的分解途径。此外，还鉴定了它们代谢产物的结构。在胸苷激酶缺陷（TK-）的CEM细胞系中，已建立了这些衍生物与它们抗HIV活性之间的相关性，其基本原理是设计能够在细胞内递送各自5'-核苷单磷酸衍生物的磷酰胺酯前药。
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