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Phosphoramidate conjugates of 3′-azido-3′-deoxythymidine glycerolipid derivatives and amino acid esters: synthesis and anti-HIV activity
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2021-01-05 , DOI: 10.1007/s00044-020-02672-8
Elizaveta S. Darnotuk , Andrei E. Siniavin , Nikolay V. Shulga , Eduard V. Karamov , Natal’ya S. Shastina

We report the synthesis of phosphoramidate conjugates of 3′-azido-3′-deoxythymidine (AZT) glycerolipid derivatives and amino acid esters. For the synthesized compounds, 50% inhibition of the HIV-1 MvP-899 strain in human T lymphoid MT-4 cells is achieved at concentrations of 0.014–0.356 µM. Significantly, compound 3c (which contained ethyl ester of α-alanine) was found to be the most active with EC50 value 0.014 µM. We show that, among these glycerolipid derivatives of AZT, some compounds are less toxic than AZT, and also they possess a similar or higher selectivity index compared to AZT (SI = 11,643).



中文翻译:

3'-叠氮基-3'-脱氧胸苷甘油脂衍生物和氨基酸酯的磷酸氨基甲酸酯偶联物:合成和抗HIV活性

我们报告了3'-叠氮基-3'-脱氧胸苷(AZT)甘油脂衍生物和氨基酸酯的氨基磷酸酯共轭物的合成。对于合成的化合物,在0.014–0.356 µM的浓度下,对人T淋巴细胞MT-4细胞中HIV-1 MvP-899菌株的抑制率为50%。显着地,发现化合物3c(包含α-丙氨酸的乙酯)最具活性,EC 50值为0.014 µM。我们显示,在AZT的这些甘油脂衍生物中,某些化合物的毒性低于AZT,并且与AZT相比,它们具有相似或更高的选择性指数(SI = 11,643)。

更新日期:2021-01-05
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