2′-Fluoro-2′,3′-Dideoxyarabinosyladenine (F-ddA): Activity against Drug-Resistant Human Immunodeficiency Virus Strains and Clades A-E-Reference-Cited by-同舟云学术

2′-Fluoro-2′,3′-Dideoxyarabinosyladenine (F-ddA): Activity against Drug-Resistant Human Immunodeficiency Virus Strains and Clades A-E

Published:1997-04 Issue:2 Volume:8 Page:107-111
ISSN:2040-2066
Container-title:Antiviral Chemistry and Chemotherapy
language:en
Short-container-title:Antivir Chem Chemother

Author:

Driscoll JS¹,Mayers DL²,Bader JP³,Weislow OS⁴,Johns DG¹,Buckheit RW⁵

Affiliation:

1. Laboratory of Medicinal Chemistry, Division of Basic Sciences, National Cancer Institute, National Institutes of Health, Building 37, Room 5C-02, Bethesda, MD 20892, USA

2. Walter Reed Army Institute of Research, 1600 East Gude Drive, Rockville, MD 20850 USA

3. Antiviral Evaluations Branch, National Cancer Institute, Executive Plaza North, Room 837, 6130 Executive Plaza Boulevard, Rockville, MD 20852, USA

4. SRA Technologies, Rockville, MD 20850, USA

5. Virology Research Group, Southern Research Institute-Frederick Research Center, Frederick, MD 21701, USA

Abstract

2′-Fluoro-2′,3′-dideoxyarabinosyladenine (F-ddA), an anti-human immunodeficiency virus (HIV) drug currently in clinical trial, was compared with zidovudine (AZT), ddl and ddC for anti-HIV activity and potency in HIV-1 strains both sensitive and resistant to zidovudine, ddl and non-nucleoside reverse transcriptase inhibitors. A variety of host cell systems [MT-2, MT-4, phytohaemagglutinin (PHA)-stimulated peripheral blood mononuclear cells (PBMC)] was used. F-ddA was effective against each of the drug-resistant isolates, including the strain resistant to ddl, the other purine dideoxynucleoside evaluated in this study. The anti-HIV-1 activities of F-ddA and zidovudine were also determined against clades A-E in PHA-PBMCs. Although activities were similar, zidovudine was significantly more potent than F-ddA in the PHA-PBMC system.

Publisher

SAGE Publications

Link

http://journals.sagepub.com/doi/pdf/10.1177/095632029700800204

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