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Title: Novel N-3 substituted TSAO-T derivatives: synthesis and anti-HIV-evaluation
Authors: Bonache, María-Cruz ×
Quesada, Ernesto
Sheen, Chih-Wei
Balzarini, Jan
Sluis-Cremer, Nicolas
Pérez-Pérez, María Jesús
Camarasa, María-José
San-Félix, Ana #
Issue Date: Apr-2008
Publisher: Marcel Dekker
Series Title: Nucleosides, Nucleotides & Nucleic Acids vol:27 issue:4 pages:351-367
Abstract: Novel derivatives of the anti-HIV-1 agent, TSAO-T, bearing at the N-3 position alkylating groups or photoaffinity labels were prepared and evaluated for their anti-HIV activity. All of these compounds demonstrated pronounced anti-HIV-1 activity and inhibited HIV-1 RT; however, we were unable to detect stable covalent linkages between inhibitor and enzyme. In addition, compounds with an alcohol functional group connected to the N-3 position through a cis or trans double bond have been prepared. These compounds have been useful to study how the conformational restriction of the linker affects in the interaction between the N-3 substituent and the HIV-1 RT enzyme.
ISSN: 1525-7770
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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