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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Official URL: http://dx.doi.org/10.1016/j.bmcl.2014.03.092
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: | Schools > Pharmacy Research Institutes & Centres > 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: | 19 Nov 2024 12:30 |
| URI: | https://orca.cardiff.ac.uk/id/eprint/59757 |
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