Cyclo-Saligenyl-3′-Azido-2′,3′-Dideoxy- Thymidinemonophosphate (cycloSal-AZTMP) - A New Pro-Nucleotide Approach1 ?-

Chris Meiera; De Clercq Erik; Jan Balzarini

doi:10.1080/07328319708002953

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Cyclo-Saligenyl-3′-Azido-2′,3′-Dideoxy- Thymidinemonophosphate (cycloSal-AZTMP) - A New Pro-Nucleotide Approach1 ?-

Article 1997 fr

Abstract

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Abstract The synthesis of cycloSal-AZTMPs 3a-h as new pro-nucleotides of AZTMP 2 is described. Phosphotriesters 3 selectively release AZTMP 2 by a controlled, chemically induced tandem reaction. CycloSal-AZTMPs 3 exhibited high biological activity in HIV-1/HIV-2 infected CEM/O cells but lost their activity nearly completely in CEM/TK- cells.

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<i>Cyclo</i>-Saligenyl-3′-Azido-2′,3′-Dideoxy- Thymidinemonophosphate (<i>cyclo</i>Sal-AZTMP) - A New Pro-Nucleotide Approach<sup>1</sup> ?-

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