齐多夫定（AZT）、司他夫定（d4T）和双脱氧腺苷（ddA）新型膦酸酯衍生物的抗HIV活性

Anti-HIV activity of novel phosphonate derivatives of AZT, d4T, and ddA.

作者信息

Pokrovsky A G, Pronayeva T R, Fedyuk N V, Shirokova E A, Khandazhinskaya A L, Tarusova N B, Karpenko I L, Krayevsky A A

机构信息

SRC Virology and Biotechnology Vector, Koltsovo, Russia, 630059.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2001 Apr-Jul;20(4-7):767-9. doi: 10.1081/NCN-100002426.

DOI:10.1081/NCN-100002426

PMID:11563112

Abstract

Anti-HIV activity and cytotoxicity were tested for novel phosphonate derivatives of AZT, d4T and ddA. For d4T phosphonate derivatives the most active was 2',3'-Dideoxy-2',3'-didehydrothymidine 5'-isopropylphosphite and among the AZT phosphonate derivatives highest activity was shown by 2',3'-Dideoxy-3'-azidothymidine 5'-cyclohexylphosphite.

摘要

对叠氮胸苷（AZT）、双脱氧胸苷（d4T）和双脱氧腺苷（ddA）的新型膦酸酯衍生物进行了抗HIV活性和细胞毒性测试。对于d4T膦酸酯衍生物，活性最高的是2'，3'-双脱氧-2'，3'-双脱氢胸苷5'-异丙基亚磷酸酯；在AZT膦酸酯衍生物中，2'，3'-双脱氧-3'-叠氮胸苷5'-环己基亚磷酸酯表现出最高活性。