The field of chemical biology has been revolutionized by click chemistry due to its remarkable efficiency, selectivity, and gentle reaction conditions. Among the various click reactions, the copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) has emerged as the most widely used technique. The formation of 1,2,3-triazoles through copper(I)-catalyzed reactions between azides and terminal acetylenes serves as an effective method for creating important medicinal frameworks. This process is highly reliable, completely specific, and utilizes biocompatible reagents. Click chemistry has emerged as a valuable approach for developing potential anticancer drug candidates. The present review highlights the recent advancements (2020-2025) in the click chemistry approach (CuAAC) for the construction of biologically important triazole moieties and their hybrid compounds as anticancer agents.