Design and synthesis of DNA-intercalating 9-fluoren-beta-O-glycosides as potential IFN-inducers, and antiviral and cytostatic agents |
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Authors: | Alcaro S Arena A Neri S Ottanà R Ortuso F Pavone B Vigorita M G |
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Affiliation: | Dipartimento di Scienze Farmacobiologiche, Università di Catanzaro 'Magna Graecia', Complesso Ninì Barbieri - 88021 Roccelletta di Borgia (CZ), Italy. |
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Abstract: | Novel 9-fluoren-beta-O-glycosides, designed as DNA-intercalating agents in structural correlation with antiviral tilorone and anticancer anthracyclines, have been prepared with yields in beta-anomers ranging between 25 and 63%. They have been screened for antiproliferative, immunostimulating and antiviral properties against HSV-1 and HSV-2 viruses. Compounds displaying significant antiviral activity against HSV-2 are acetylated 1 and deprotected 6 9-fluorenyl-O-d-arabinopyranoses, whereas 9-fluorenyl-O-d-glucopyranose 3 is the most effective on HSV-1 replication, followed by 1 and 6. The conformational properties of these compounds have been evaluated by molecular modelling techniques. |
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