Synthesis and anticancer potential of glycosides

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Abstract

Cancer drug development faces significant challenges, primarily owing to the resistance of cancer cells. Recent efforts have focused on creating drugs with effective IC50 values and acceptable cytotoxicity standards as defined by organizations such as the IARC, UICC, AACR, WHO, and NCI. The synthesis of S-, N-, C-, and O-glycosidic linkages, protection of the glucose moiety, and modification tactics via alkylation, acylation, and esterification, α-glycosyl imidate formation, glycosyl radical functionalization, CuAAC reaction, and tagging and editing methods are also investigated. These efforts have streamlined the progress in the production of glycosidic compounds as antitumour agents because of their effectiveness and potency in MDR cancer cell lines. Despite their ultra-features, advanced cytotoxic analysis with robotics requires a deep understanding of their kinetics, which are studied by employing FID, TUNEL, ELISA, FRET, DNA cleavage, caspase, linear regression, and SRB assays. Meanwhile, the synthesised products were characterized using micro-FTIR, UFLC-DAD, cryogenic electron microscopy, elemental analysis, and molecular imaging techniques. Docking simulation, molecular dynamics simulations, and QSAR analyses helped in understanding the binding of the designed compounds to the active sites of the targeted cells. In this perspective, we explored the essential role of glycosidic compounds in synthesizing target-based drugs and their application in cancer treatment.

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Ali, S., Rukh, G., Ogaly, H. A., Ajaj, R., Rauf, A., & Ali Shah, S. A. (2025). Synthesis and anticancer potential of glycosides. RSC Advances. Royal Society of Chemistry. https://doi.org/10.1039/d5ra07626a

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