Design, Synthesis, Evaluation And Molecular Docking Studies Of 1,6-Bis-Triazole-Linked Alpha-Galactoside Derivatives As Potential Anticancer Agents

A series of novel 1,6-bis-triazole-linked alpha-galactoside derivatives (5 a-5 bb) were designed and synthesized in high yields through O-Glycosylation and click chemistry. All analogues were evaluated for their in vitro cytotoxic activity against nine cancer cell lines. Cytotoxicity results demonstrate that compounds 5 o and 5 bb showed significant cytotoxic activities against leukemia (P-388, IC50=4.45 mu M) and cholangiocarcinoma (K-100, IC50=4.87 mu M) cancer cells. Molecular docking studies of active compounds displayed good binding energies towards both CDK-2 and EGFR proteins, correlated with their in vitro results.