In recent years, there has been a crucial need for the design and development of novel anticancer drugs which can lessen serious health problems and unwanted side effects associated with currently used anticancer drugs. Triazole nucleus is well-recognized to possess numerous pharmacological activities including anticancer as revealed from various investigations on anticancer drugs and latest research findings. This review provides an overview of anticancer potentiality of 1, 2, 3-triazole, 1, 2, 4-triazole and heterocycle-fused triazole derivatives, particularly, 1,2,3-triazole coupled oleanolic acid/ dithiocarbamate/ pyrido[2,3-d]pyrimidine derivatives, 1,2,3-triazole linked pyrimidine/1,4-naphthoquinone hybrids and 1,2,4-triazole substituted methanone derivatives, acridine-based 1,2,4-triazole derivatives, 1,2,4-thiadiazol coupled 1,2,4-triazole and 5-ene-thiazolo[3,2-b][1,2,4]triazole-6(5H)-one derivatives against several human cancer cell lines, compiling research articles published between 2010 and 2021.