Selective inhibition of human immunodeficiency virus type 1 replication by novel fluoroalkylated oligomers in vitro.
Several fluoroalkylated oligomers were found to be potent and selective inhibitors of human immunodeficiency virus type 1 (HIV-1) in vitro. Among the test compounds, bis(perfluoro-1,4,7,10-tetramethyl-2,5,8,11-tetraoxatetradecyl+ ++)methacrylic acid oligomer (MAA-HFPO5) emerged as the most potent inhibitor of HIV-1 replication. Its 50% antivirally effective concentration for the IIIB strain was 2.8 mu g/ml, whereas the compound did not affect the growth and viability of mock-infected MT-4 cells at concentrations < or = 100 micrograms/ml. MAA-HFPO5 was also inhibitory to other strains of HIV-1 in various human T-cell systems, including peripheral blood lymphocytes. MAA-HFPO5 inhibited syncytium formation and virus adsorption. The combination of MAA-HFPO5 with either 3'-azido-3'dioxythymidine or dextran sulfate resulted in an additive effect. Thus, fluoroalkylated oligomers are novel HIV-1 inhibitors that warrant further evaluation of their therapeutic potential.
Baba
M
M
Department of Microbiology, Fukushima Medical College, Japan.
Kira
T
T
Shigeta
S
S
Matsumoto
T
T
Sawada
H
H
D000327:Adsorption / Q000187:drug effects; D002460:Cell Line; D003588:Cytopathogenic Effect, Viral / Q000187:drug effects; D016264:Dextran Sulfate / Q000494:pharmacology; D004347:Drug Interactions; D005466:Fluorocarbons / Q000737:chemistry / Q000494:pharmacology*; D015726:Giant Cells / Q000187:drug effects; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D014779:Virus Replication / Q000187:drug effects*; D015215:Zidovudine / Q000494:pharmacology
D005466:Fluorocarbons; D015215:Zidovudine; D016264:Dextran Sulfate