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Title: Effect of human serum on the in vitro anti-HIV-1 activity of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) derivatives as related to their lipophilicity and serum protein binding
Authors: Baba, M ×
Yuasa, S
Niwa, T
Yamamoto, M
Yabuuchi, S
Takashima, H
Ubasawa, M
Tanaka, H
Miyasaka, T
Walker, R T
Balzarini, Jan
De Clercq, Erik
Shigeta, S #
Issue Date: 19-Aug-1993
Series Title: Biochemical Pharmacology vol:45 issue:12 pages:2507-12
Abstract: Several derivatives of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) were examined for their inhibitory effects on the replication of human immunodeficiency virus type 1 (HIV-1) in MT-4 cells in the presence of various concentrations (10-50%) of human serum (HS). Although all HEPT derivatives proved to be highly potent inhibitors of HIV-1 in the presence of 10% fetal bovine serum, some of them were less inhibitory to HIV-1 replication in the presence of HS. The HEPT derivatives were found to be highly bound to HS proteins. Both the anti-HIV-1 activity and HS protein binding of the compounds appeared to be related to their lipophilicity.
ISSN: 0006-2952
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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