Shirokova Elena A, Jasko Maxim V, Khandazhinskaya Anastasiya L, Ivanov Alexander V, Yanvarev Dmitry V, Skoblov Yury S, Mitkevich Vladimir A, Bocharov Eduard V, Pronyaeva Tatyana R, Fedyuk Nina V, Kukhanova Marina K, Pokrovsky Andrey G
Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, 32 Vavilov str., Moscow 119991, Russian Federation.
J Med Chem. 2004 Jul 1;47(14):3606-14. doi: 10.1021/jm0310176.
Two series of new lipophilic phosphonoformate and phosphonoacetate derivatives of AZT and d4T were synthesized and evaluated as anti-HIV agents. The efficacy of some of the synthesized compounds in cell cultures infected with HIV-1 was higher than that of the parent nucleosides and only slightly correlated to their stability in the phosphate buffer and human blood serum. The synthesized phosphonates are most probably prodrug forms of the corresponding nucleosides.
合成了两系列新的齐多夫定（AZT）和司他夫定（d4T）的亲脂性膦甲酸酯和膦乙酸酯衍生物，并作为抗HIV药物进行了评估。一些合成化合物在感染HIV-1的细胞培养物中的疗效高于母体核苷，且与它们在磷酸盐缓冲液和人血清中的稳定性仅有微弱关联。合成的膦酸酯很可能是相应核苷的前药形式。
