Synthesis and Biological Evaluation of Triazolylnucleosides as Antibacterial and Anticancer Agents

Abstract A series of novel triazolylnucleosides has been efficiently synthesized (6a-h, 7a-b) by azide–alkyne 1,3-dipolar cycloaddition reaction and evaluated for antibacterial and anticancer activities. These nucleosides (6a-h) were screened against Staphylococcus aureus (ATCC 6538), gram-positive and Escherichia coli (ATCC 10536), Salmonella and Pseudomonas gram-negative bacterial strains. Among the series, three compounds (6c-e) exhibited significant levels of antibacterial activity against Staphylococcus aureus in reference to the standard drug, Levofloxacin. Triazolylnucleosides (6a-h) were also screened for anti-proliferative activities against cancer cell lines such as Huh-7 liver cancer cells. Three compounds (6e, 7a-b) have displayed promising anti-proliferative activity against Huh-7 and U87G cancer cells lines.