1,2,3-Triazole moiety which is usually constructed by highly versatile, efficacious and selective copper-catalyzed azide-alkyne cycloaddition not only can act as a linker to connect different pharmacophores, but also is a useful pharmacophore with diverse biological properties. 1,2,3-Triazoles are readily interact with diverse enzymes and receptors in cancer cells through non-covalent interactions and can inhibit cancer cell proliferation, arrest cell cycle and induce apoptosis. In particular, 1,2,3-triazole-containing hybrids have the potential to exert dual or multiple anticancer mechanisms of action, representing useful scaffolds in expediting development of novel anticancer agents. The current review summarizes the in vivo anticancer efficacy and mechanisms of action of 1,2,3-triazole-containing hybrids reported in the last decade to continuously open up a map for the remarkable exploration of more effective candidates.