Benzothiazole is an aromatic heterocyclic compound with the chemical formula of C7H5NS. Benzothiazole: Preparation, Structure and Uses opens with a review on the synthesis of benzothiazoles for their anticancer, antimicrobial, antidiabetic, anticonvulsant, anti-inflammatory, anthelmintic, analgesic, antiviral and antitubercular activities. Following this, considering the versatile nature of benzothiazole, various benzothiazole derivatives with anticonvulsant and anticancer activity are discussed in detail. A report on the design strategies, detailed photo-physical properties and applications of benzothiazoles is provided in an effort to help researchers overcome existing challenges in designing novel excited state intramolecular proton transfer benzothiazole fluorescent molecules. In closing, the authors present recent updates on the usefulness and structure-activity relationship of benzothiazole derivatives for the development of novel anticancer agents.