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Selective Inhibition of Human Immunodeficiency Virus Type 1 Replication by Novel Fluoroalkylated Oligomers In Vitro

 

作者: Masanori Baba,   Toshihiko Kira,   Shiro Shigeta,   Takeo Matsumoto,   Hideo Sawada,  

 

期刊: Journal of Acquired Immune Deficiency Syndromes  (OVID Available online 1994)
卷期: Volume 7, issue 1  

页码: 24-30

 

ISSN:0894-9255

 

年代: 1994

 

出版商: OVID

 

关键词: HIV-1;Chemotherapy;Fluorine;Polymer;Antiviral activity.

 

数据来源: OVID

 

摘要:

SummarySeveral 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 IIIBstrain was 2.8 g/ml, whereas the compound did not affect the growth and viability of mock-infected MT-4 cells at concentrations $100 μg/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.

 

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