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  • Title: From β-amino-γ-sultone to unusual bicyclic pyridine and pyrazine heterocyclic systems: synthesis and cytostatic and antiviral activities.
    Author: de Castro S, Familiar O, Andrei G, Snoeck R, Balzarini J, Camarasa MJ, Velázquez S.
    Journal: ChemMedChem; 2011 Apr 04; 6(4):686-97. PubMed ID: 21370477.
    Abstract:
    Herein we describe the first successful application of the β-amino-γ-sultone system as an intermediate for the synthesis of hitherto virtually unknown 3H-[1,2]-oxathiole [4,3-b]pyridine and pyrazine 1,1-dioxide bicyclic heterocyclic systems. All novel compounds were evaluated for their antiviral and cytostatic activities. Compounds 3 a, 15 a, and 21 a inhibited HIV-1-induced cytopathicity. Compound 7 showed remarkable cytostatic activity, and can be regarded as a potential antitumor candidate for further exploration.
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