Enhanced in vitro inhibition of HIV-1 replication by 3'-fluoro-3'-deoxythymidine compared to several other nucleoside analogs.
Nucleoside analogs were synthesized and tested for anti-HIV-1 activity in two in vitro test systems using MT-4 cells and peripheral blood lymphocytes. Cytotoxicity was assessed in both assays and additionally in several human lymphoblastoid cell lines. One analog, 3'-fluoro-3'-deoxythymidine, exhibited higher antiviral potency and slightly higher cytotoxicity than 3'-azido-3'-deoxythymidine. Analogs showing lower cytotoxicity than 3'-azido-3'-deoxythymidine demonstrated reduced antiviral activity. 3'-fluoro-3'-deoxythymidine may become an alternative chemotherapeutic agent because of its high antiretroviral potency. Its toxicity, however, deserves further investigation.
Hartmann
H
H
Deutsches Primatenzentrum GmbH, Abt. Virologie und Immunologie, Göttingen, FRG.
Vogt
M W
MW
Durno
A G
AG
Hirsch
M S
MS
Hunsmann
G
G
Eckstein
F
F
D002460:Cell Line; D015224:Dideoxynucleosides / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D066298:In Vitro Techniques; D007963:Leukocytes, Mononuclear; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D013936:Thymidine / Q000031:analogs & derivatives* / Q000494:pharmacology; D014779:Virus Replication / Q000187:drug effects*; D015215:Zidovudine / Q000031:analogs & derivatives / Q000494:pharmacology
D015224:Dideoxynucleosides; D015215:Zidovudine; C002854:alovudine; D013936:Thymidine