Synthesis and DNA topoisomerase-II inhibitory activity of unnatural nucleosides

Article abstract of DOI:10.1081/NCN-200046776

The synthesis and biological activities of a number of unnatural nucleosides (23-43) is described. Nucleosides have been synthesized by SnCl ₄-catalyzed condensation of amino sugar acetates and silylated modified pyrimidines. Few of the 2′-O-acetyl derivatives of the nucleosides were hydrolyzed to the respective hydroxy derivatives by treatment with methanol saturated with ammonia. The compounds were screened against Filarial DNA-topoisomerase-II but only one of the compounds (29) inhibited this enzyme at 40 μg/mL of reaction mixture.