Synthesis of 5-alkynylated d4T analogues as potential HIV-1 reverse transcriptase inhibitors |
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| Authors: | Ciurea A Fossey C Gavriliu D Delbederi Z Sugeac E Laduree D Schmidt S Laumond G Aubertin A M |
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| Affiliation: | Centre d'Etudes et de Recherche sur le Médicament de Normandie, UFR des Sciences Pharmaceutiques, F-14032 Caen Cedex, France. |
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| Abstract: | A series of 2',3'-didehydro-2',3'-dideoxynucleosides substituted with an alkynylhydroxy- (6, 7, 12 and 13) and alkynylamino- (20) groups at the C-5 position were synthesized. All these five target modified nucleosides were tested for anti-human immunodeficiency virus type 1 activity in CEM-SS and MT-4 cells and unfortunately displayed no improvement in antiviral activity. |
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