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Título: | Synthesis and Anti-HIV Activity of [UT]-[TSAO-TI and [UT]-[HEPT] Dimers as Potential Multifunctional Inhibitors of HIV-1 Reverse Transcriptase |
Autor: | Velázquez, Sonsoles CSIC ORCID CVN; Álvarez, Rosa; San-Félix, Ana CSIC ORCID ; Jimeno, M. Luisa CSIC ORCID; De Clercq, Erik; Camarasa Rius, María José CSIC ORCID | Fecha de publicación: | 1995 | Editor: | American Chemical Society | Citación: | Journal of Medicinal Chemistry 38 : 1641-1649 (1995) | Resumen: | In an attempt to combine the HIV-inhibitory capacity of 2',3'-dideoxynucleoside (ddN) analogues and non-nucleoside reverse transcriptase (RT) inhibitors (NNRTI), we have designed, synthesized, and evaluated for their anti-HIV activity several dimers of the general formula [ddNl- (CH2),-[NNRTIl. These dimers combine in their structure a ddN such as AZT and a NNRTI such as TSAO-T and HEPT linked through an appropriate spacer between the N-3 of the thymine base of both compounds. The [TSAO-Tl-(CH2),-[AZTl dimers proved markedly inhibitory to HIV-1. Also, if AZT was replaced by thymidine in the dimer molecules, potent anti-HIV-1 activity was observed. However, although the compounds proved inhibitory to HIV- 1, they were less potent inhibitors than the parent compounds from which they were derived. None of the dimers were endowed with anti-HIV-2 activity. In contrast with the TSAO-T monomers, none of the TSAO-T-containing dimers proved markedly cytotoxic to the cells. There was a clear trend toward decreased antiviral potency with lengthening the methylene spacer in the [TSAO-Tl-(CH2),-[AZTl dimers | Versión del editor: | http://dx.doi.org/10.1021/jm00010a008 | URI: | http://hdl.handle.net/10261/37923 | DOI: | 10.1021/jm00010a008 | ISSN: | 0022-2623 | E-ISSN: | 1520-4804 |
Aparece en las colecciones: | (CENQUIOR) Artículos |
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