Synthesis and Biological Activity of Substituted Benzothiazole Derivatives

Despite improvements in survival rates, cancer and viral diseases remain the second leading cause of death in the western world. Therefore, an area of major pharmaceutical interest over the last several decades has been the development of small molecules with antitumor and antiviral activity. Two potential targets for compounds with antitumor and antiviral activity are DNA and different types of proteins like tyrosine kinases or topoisomerase I/II. Therefore, the design of new intercalators, groove-binders and discovery of specific inhibitors of proteins are two important approaches in the search for new chemotherapeutic agents. Over the past decade, development of small heterocyclic molecules as potential therapeutics has been an area of major interest. A large number of benzothiazole derivatives are of considerable biological and chemical interest. In the last several decades there has been a significant increase in the preparation of benzothiazole derivatives and their biological activity. Many 2-substituted benzothiazoles have been reported to display a large panel of biochemical properties, including antibacterial, antitumor, antiviral and antibiotic activities. Variation of substituents on the benzothiazole nuclei could potentially affect the interaction of the molecules with biological targets. Benzothiazole compounds received much attention from medicinal as well as synthetic organic chemists, not just due to their potential as biologically active compounds, but also as tools to study and visualize DNA. Because of their capacity to penetrate through cell membranes they were proposed for DNA visualization in fluorescent microscopy. These types of compounds are also interesting because of their applications in several areas as materials in electronics, as optical polymers and as anticorrosive protection.