Key Heterocyclic Cores for Smart Anticancer Drug–Design Part I

Recent Advances in Synthesis and the Anticancer Activity of Benzothiazole Hybrids as Anticancer Agents

Author(s): Rajesh Kumar*, Monika Sharma, Sarita Sharma and Rajesh K. Singh * .

Pp: 105-166 (62)

DOI: 10.2174/9789815040074122010006

* (Excluding Mailing and Handling)


Cancer is known as a silent killer that wreaks havoc on our immune systems. Cancer is the leading cause of death in the majority of cases. Resistance to anticancer drugs is becoming more agile, which encourages researchers to develop more effective cancer therapies. Heterocyclic compounds have long been important in advanced medicinal chemistry. Among the various heterocyclic scaffolds, benzothiazole (BT) is one of the most privileged moieties with a diverse range of biological activities such as anticancer, antidiabetic, anti-inflammatory, antiviral, antifungal, and so on. A large number of novel benzothiazole derivatives have been synthesized. Some of the mechanisms used by BT to treat cancer include tyrosine-kinase inhibitors, topoisomerase II inhibitors, CYP450 enzyme inhibitors, Abl kinase inhibitors, tubulin polymerase inhibitors, and HSP90 inhibitors. In this chapter, we will discuss various benzothiazole-hybrid compounds that optimise potency as well as anticancer activity in a concise manner. The goal of this chapter is to highlight recent research on benzothiazole scaffolds and their anticancer activity against various biological targets. The chapter will also provide updates on benzothiazole-containing drugs that are currently in clinical trials as well as those that have recently been granted patents. 

Keywords: Anticancer activity, Benzothiazole, Bio targets, Heterocyclic scaffold, Structure-activity relationship (SAR), Synthesis.

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