Design, Synthesis, Evaluation and Molecular Docking Studies of 1,6-Bis-triazole-Linked α-Galactoside Derivatives as Potential Anticancer Agents

Suksamran ChaidamNatthiya SaehlimKanoknetr SuksenArthit ChairoungduaRungnapha SaeengMahidol UniversityBurapha University2022-08-042022-08-042021-08-20ChemistrySelect. Vol.6, No.31 (2021), 8052-8057236565492-s2.0-85113536014https://repository.li.mahidol.ac.th/handle/20.500.14594/76597A 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.Mahidol UniversityChemistryDesign, Synthesis, Evaluation and Molecular Docking Studies of 1,6-Bis-triazole-Linked α-Galactoside Derivatives as Potential Anticancer AgentsArticleSCOPUS10.1002/slct.202102288