Heterocyclic compounds, analogs and derivatives have attracted attention due to their diverse
biological and pharmacological properties. Benzoheterocycles such as
benzothiazoles,
benzimidazoles and
benzoxazoles are constituents of many bioactive
heterocyclic compounds, having wider range of applications. They have been extensively studied for their
biological activities, and can serve as unique and versatile scaffolds for
drug design. The
benzothiazole, in the family of
heterocyclic compounds has assumed special significance in synthetic chemistry, pharmaceutical chemistry as well as in clinical applications because of its anti-
tumor properties. This review is organized in the following ways. It begins with brief introduction on the chemical diversity of synthetic analogs of
benzothiazole. After this,
drug design strategy and mechanisms of action through its diverse
biological targets in which
benzothiazole and its derivatives display their anticancer activity are discussed. It ends with the metabolism pattern of
benzothiazole and its analogs. Analysis of the structure-activity relationships (SAR), quantitative structure-activity relationships (QSAR) as well as on docking studies of this family of compounds highlights the potential that may lead to the development of novel
anticancer agents. Such relationships will definitely create lot of interest among the researchers to synthesize optimized variety of
benzothiazole derivatives and to screen them for their anticancer activity.