Synthesis, anti-HIV activity and stability studies of 3'-azido-2',3'-dideoxythymidine 5'-fluorophosphate.

D Egron, A A Arzumanov, N B Dyatkina, A Krayevsky, J L Imbach, A M Aubertin, G Gosselin, C Périgaud
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引用次数: 4

Abstract

The synthesis, in vitro anti-HIV activity, and stability studies of AZT 5'-fluorophosphate (F-AZTMP) are reported. The present results demonstrate that such compound is a bioprecursor of its parent 5'-mononucleotide (AZTMP) but its biotransformation does not allow its selective intracellular delivery. Moreover, several attempts were carried out in order to improve the biological activity of this compound by the use of a SATE prodrug strategy.

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3'-叠氮-2',3'-二脱氧胸腺嘧啶5'-氟磷酸盐的合成、抗hiv活性及稳定性研究。
本文报道了azt5′-氟磷酸盐(F-AZTMP)的合成、体外抗hiv活性和稳定性研究。目前的研究结果表明,该化合物是其亲本5'-单核苷酸(AZTMP)的生物递质,但其生物转化不允许其选择性细胞内递送。此外,为了提高该化合物的生物活性,进行了几次尝试,以使用SATE药前策略。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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