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Synthesis and Anti-HIV Activity of [UT]-[TSAO-TI and [UT]-[HEPT] Dimers as Potential Multifunctional Inhibitors of HIV-1 Reverse Transcriptase

AuthorsVelázquez, Sonsoles ; Álvarez, Rosa; San-Félix, Ana ; Jimeno, M. Luisa ; De Clercq, Erik; Camarasa Rius, María José
Issue Date1995
PublisherAmerican Chemical Society
CitationJournal of Medicinal Chemistry 38 : 1641-1649 (1995)
AbstractIn 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
Publisher version (URL)http://dx.doi.org/10.1021/jm00010a008
Appears in Collections:(CENQUIOR) Artículos
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