Issue 59, 2025

Synthesis and anticancer potential of glycosides

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.

Graphical abstract: Synthesis and anticancer potential of glycosides

Article information

Article type
Review Article
Submitted
06 Oct 2025
Accepted
20 Nov 2025
First published
19 Dec 2025
This article is Open Access
Creative Commons BY license

RSC Adv., 2025,15, 51054-51099

Synthesis and anticancer potential of glycosides

S. Ali, G. Rukh, H. A. Ogaly, R. Ajaj, A. Rauf and S. A. Ali Shah, RSC Adv., 2025, 15, 51054 DOI: 10.1039/D5RA07626A

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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