Benzothiazole is an organic compound bearing a heterocyclic nucleus (thiazole) that imparts a broad spectrum of biological activity to it. The significant and potent activity of benzothiazole moiety influenced distinctively by nature and position of substitutions. This review summarizes of the effect of various substituents in recent trends and approaches to design and develop novel benzothiazole derivatives for anticancer potential in different cell lines by interpreting the structure-activity relationship (SAR) and mechanism of action of a wide range of derivatives. The list of derivatives are categorized in different groups and reviewed for their anticancer activity. The structure-activity relationship for the various derivatives revealed an excellent understanding of benzothiazole moiety in the field of cancer therapy against different cancer cell line. Data obtained from the various articles showed the potential effect of benzothiazole moiety and its derivatives to produce the peculiar and significant lead compound. The important anticancer mechanisms found are tyrosine kinase inhibition, topoisomerase inhibition and induction of apoptosis by reactive oxygen species (ROS) activation. Therefore, the design and development of novel benzothiazole have broad scope in cancer chemotherapy.
Keywords: Benzothiazole, Anticancer, Cell line Mechanism of Action, Structure-activity relationship, Tyrosine kinase inhibition, Topoisomerase inhibition, Apoptosis
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