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

Velanguparackel, Winnie, Hamon, Nadege, Balzarini, Jan, McGuigan, Christopher and Westwell, Andrew D. 2014. Synthesis, anti-HIV and cytostatic evaluation of 3′-deoxy-3′-fluorothymidine (FLT) pro-nucleotides. Bioorganic and Medicinal Chemistry Letters 24 (10) , pp. 2240-2243. 10.1016/j.bmcl.2014.03.092

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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.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Systems Immunity Research Institute (SIURI)
Subjects: R Medicine > RS Pharmacy and materia medica
Uncontrolled Keywords: Nucleosides; Antiviral; Anticancer; Phosphoramidates; Pro-nucleotides; Pro-drugs
Publisher: Elsevier
ISSN: 0960-894X
Date of First Compliant Deposit: 30 March 2016
Last Modified: 14 Mar 2022 16:47

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