SELECTIVE-INHIBITION OF HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 REPLICATION BY NOVEL FLUOROALKYLATED OLIGOMERS IN-VITRO

Several fluoroalkylated oligomers were found to be potent and selectiv e inhibitors of human immunodeficiency virus type 1 (HIV-1) in vitro. Among the test compounds, etramethyl-2,5,8,11-tetraoxatetradecyl)metha crylic 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 t he growth and viability of mock-infected MT-4 cells at concentrations less than or equal to 100 mu g/ml. MAA-HFPO5 was also inhibitory to ot her strains of HIV-1 in various human T-cell systems, including periph eral blood lymphocytes. MAA-HFPO5 inhibited syncytium formation and vi rus adsorption. The combination of MAA-HFPO5 with either 3'-azido-3'di oxythymidine or dextran sulfate resulted in an additive effect. Thus, fluoroalkylated oligomers are novel HIV-1 inhibitors that warrant furt her evaluation of their therapeutic potential.