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

Velanguparackel, Winnie, Hamon, Nadege, Balzarini, Jan, McGuigan, Christopher ORCID: https://orcid.org/0000-0001-8409-710X and Westwell, Andrew D. ORCID: https://orcid.org/0000-0002-5166-9236 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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Abstract

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:	10 Nov 2023 17:37
URI:	https://orca.cardiff.ac.uk/id/eprint/59757

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