Synthesis, Molecular Docking And Anticancer Activity Of New Substituted Pyridine1,2,3-Triazole Hybrid N-Glycosides Via Click Chemistry

Cancer is still the most upsetting threat for human life and its fighting strategies have acquired intensive research. The design and synthesis of novel candidates for their possible potent anticancer activity has become a major objective in the drug anticancer discovery field. In the current research, new 1,2,3-triazole glycosides linked to substituted pyridine system were prepared vis click chemistry approach. A number of substituted acetylenic substrates incorporating varied structural features were applied for the click reaction. Various sugar moieties as acetylated glycopyranosyl forms provided the 1,4-disubstituted 1,2,3-triazole products possessing sugar, aryl- or heteroaryl substituents in the synthesized compounds. The 1,2,3-triazole glycoside 10 and its acetylenic precursor 6 possessing the biphenyl and thienyl rings in addition to the O-acetylated glucopyranosyl moiety showed the highest activity against A549, MCF7 and PC3 human cancer cell lines. Furthermore, the docking studies into EGFR and EGFR showing good binding modes with the protein active sites.