Title: First synthesis and evaluation of the inhibitory effects of aza analogues of TSAO on HIV-1 replication
Authors: Van Nhien, Albert ×
Tomassi, Cyrille
Len, Christophe
Marco-Contelles, José Luis
Balzarini, Jan
Pannecouque, Christophe
De Clercq, Erik
Postel, Denis #
Issue Date: Jun-2005
Publisher: ACS Publications
Series Title: Journal of Medicinal Chemistry vol:48 issue:13 pages:4276-4284
Abstract: Aza TSAO-T derivatives bearing a dihydroisothiazole dioxide ring instead of an oxathiole dioxide ring at the C-3' position on the sugar moiety were prepared. We have synthesized four families of compounds depending on substitution at both N-3 and N-2' '. Biological evaluation showed that these compounds are HIV-1(III(B))-specific and potent reverse transcriptase inhibitors with EC(50) values between 0.13 and 3.5 microM in cell culture.
ISSN: 0022-2623
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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