Benzothiazole is a versatile fused heterocyclic scaffold with extensive pharmaceutical applications. Several benzothiazole derivatives possess broad spectrum of antimicrobial, analgesic, anti-inflammatory, antidiabetic activities and so on, and the structurally simple 2-arylbenzothiazoles are potential antitumor agents. Some of the compounds containing benzothiazole ring system are in clinical usage for the treatment of various diseases/disorders.In the present review, the authors summarize inventions carried out towards the development of benzothiazole-based chemotherapeutic agents. It provides an overview of the patents filed during 2010 - 2014 pertaining to the anticancer, antimicrobial, anti-inflammatory and other biological activities of benzothiazole derivatives.Several molecules containing benzothiazole skeleton are agents of choice for the treatment of various human diseases/disorders. Its versatile character of being capable of serving as ligand to various biomolecules attracted the interest of medicinal chemists for the development of therapies for respective ailments, especially, the 2-arylbenzothiazole moiety which is under development for the treatment of cancer. This signifies the increasing importance of benzothiazole nucleus in the area of drug discovery. Its structural simplicity and ease of synthesis provides scope for the development of chemical libraries that could serve in the discovery of new chemical entities progressing towards the market.