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Novel N-3 substituted TSAO-T derivatives: Synthesis and anti-HIV-evaluation

AuthorsBonache, María-Cruz ; Quesada, Ernesto ; Sheen, C.-W.; Balzarini, Jan; Sluis-Cremer, N.; Peréz-Pérez, María-Jesús ; Camarasa Rius, María José ; San-Félix, Ana
Issue Date2008
PublisherMarcel Dekker
CitationNucleosides, Nucleotides and Nucleic Acids 27: 351- 367 (2008)
AbstractNovel 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. Copyright © Taylor & Francis Group, LLC.
Identifiersdoi: 10.1080/15257770801943990
issn: 1525-7770
e-issn: 1532-2335
Appears in Collections:(IQM) Artículos
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