New Phosphonoformic Acid Derivatives of 3′-Azido-3′-Deoxythymidine

被引:0
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作者
E. A. Shirokova
M. V. Jasko
A. L. Khandazhinskaya
A. V. Ivanov
D. V. Yanvarev
Yu. S. Skoblov
T. R. Pronyaeva
N. V. Fedyuk
A. G. Pokrovskii
M. K. Kukhanova
机构
[1] Russian Academy of Sciences,Engelhardt Institute of Molecular Biology
[2] Vector State Research Center of Virology and Biotechnology,undefined
关键词
3′-azido-3′-deoxythymidine; human immunodeficiency virus; nucleoside phosphonates;
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摘要
New 5′-alkyl ethoxy- and aminocarbonylphosphonates of 3′-azido-3′-deoxythymidine (AZT) were synthesized, and their antiviral properties in HIV-1-infected cell cultures and stability to chemical hydrolysis were studied. The AZT 5′-aminocarbonylphosphonates were shown to be significantly more stable in phosphate buffer (pH 7.2) than the corresponding ethoxycarbonylphosphonates. The therapeutic (selectivity) index of some of the compounds exceeded that of the parent AZT due to their higher antiviral activity.
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页码:242 / 249
页数:7
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