Synthesis, anti-HIV and cytostatic evaluation of 3′-deoxy-3′-fluorothymidine (FLT) pro-nucleotides

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:24

Article

Velanguparackel, Winnie¹  Hamon, Nadege¹  Balzarini, Jan²  McGuigan, Christopher¹  Westwell, Andrew D.¹ 

[1] Cardiff Univ, Sch Pharm & Pharmaceut Sci, Cardiff CF10 3NB, S Glam, Wales

[2] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium

关键词: Nucleosides;    Antiviral;    Anticancer;    Phosphoramidates;    Pro-nucleotides;    Pro-drugs;   

DOI  :  10.1016/j.bmcl.2014.03.092

来源: Elsevier

【 摘 要 】

A series of pro-nucleotide phosphoramidates and phosphorodiamidates of the antiviral lead compound 3 '-deoxy-3 '-fluorothymidine (FLT) have been designed and synthesized. In vitro antiretroviral and cytostatic studies revealed potent (sub-micromolar) inhibition of HIV-1 and HIV-2 replication, with retention of activity in thymidine kinase-negative cell models, as predicted by the ProTide concept. (C) 2014 Elsevier Ltd. All rights reserved.

【 授权许可】

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