Synthesis of 4′-Thionucleosides as Antitumor and Antiviral Agents

抄録

Many attempts have been made to synthesize structurally novel nucleoside derivatives in order to identify effective compounds for the treatment of tumors and virus-caused disease. At our laboratories, as part of our efforts to synthesize 4′-thionucleosides, we have identified and characterized biologically active nucleosides. During the course of our synthetic study, we developed the Pummerer-type thioglycosylation reaction. As a result, we synthesized a potent antineoplastic nucleoside, 1-(2-deoxy-2-fluoro-β-D-4-thio-arabino-furanosyl)cytosine (4′-thioFAC), and several novel 4′-thionucleosides that possess antiherpes virus activities.