edoc

Thiated derivatives of 2',3'-dideoxy-3'-fluorothymidine : synthesis, in vitro anti-HIV-1 activity and interaction with recombinant drug resistant HIV-1 reverse transcriptase forms

Miazga, Agnieszka and Hamy, François and Louvel, Séverine and Klimkait, Thomas and Pietrusiewicz, Zofia and Kurzy?ska-Kokorniak, Anna and Figlerowicz, Marek and Wi?ska, Patrycja and Kulikowski, Tadeusz. (2011) Thiated derivatives of 2',3'-dideoxy-3'-fluorothymidine : synthesis, in vitro anti-HIV-1 activity and interaction with recombinant drug resistant HIV-1 reverse transcriptase forms. Antiviral research, Vol. 92, H. 1. pp. 57-63.

Full text not available from this repository.

Official URL: http://edoc.unibas.ch/dok/A6005085

Downloads: Statistics Overview

Abstract

Various thiated analogues of thymine 2',3'-dideoxy-3'-fluoronucleoside (FLT) and their 5'-monophosphates and 5'-triphosphates were prepared with the use of modified multistep procedures. The thiated analogues of FLT and FLTMP were evaluated against the wild type and drug- and multidrug-resistant strains of HIV-1, using the replicative phenotyping format of the deCIPhR assay, and showed potent inhibition of drug-resistant HIV-1 strains at low cytotoxicity. Additionally, inhibition of recombinant drug resistant forms of reverse transcriptase from single and multiple HIV-1 mutants by the synthesized 5'-triphosphates was investigated. The strongest inhibition was observed for K103N and ?67 mutants and the most potent anti-HIV-1 activity against drug resistant strains and the lowest cytotoxicity was exerted by S4FLTMP and FLTMP which may be regarded as potential anti-HIV/AIDS agents.
Faculties and Departments:03 Faculty of Medicine > Departement Biomedizin > Division of Medical Microbiology > Molecular Virology (Klimkait)
UniBasel Contributors:Klimkait, Thomas
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:Elsevier
ISSN:0166-3542
Note:Publication type according to Uni Basel Research Database: Journal article
Related URLs:
Identification Number:
Last Modified:08 May 2015 08:44
Deposited On:06 Dec 2013 09:36

Repository Staff Only: item control page