Cancer remains prevalent for the significant healthcare concern worldwide urging the development of efficient, selective and less toxic anticancer agents. The benzothiazole nucleus, particularly 2-Aminobenzothiazole having a heterocyclic structure with sulfur and nitrogen atom, has been investigated widely due to its broad spectrum of pharmacological activities including anticancer, antimicrobial, anti-inflammatory and other properties. This article reviews the anticancer potential of benzothiazole scaffold encompassing the chemical structure, structural activity relationship from different derivatives. Various synthesis methods and the pharmacological properties exhibited by the benzothiazole derivatives with special emphasis on anticancer activity are extensively reviewed.