A series of novel 1,6-bis-triazole-linked α-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 μM) and cholangiocarcinoma (K-100, IC50=4.87 μM) 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.
