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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, Álvarez, Rosa, San-Félix, Ana, Jimeno, M. Luisa, De Clercq, Erik, Camarasa Rius, María José
Fecha de publicación : 1995
Editor: American Chemical Society
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
ISSN: 0022-2623
DOI: 10.1021/jm00010a008
Citación : Journal of Medicinal Chemistry 38 : 1641-1649 (1995)
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