As one of the leading causes of deaths worldwide, cancer is posing threat despite efforts being
taken to develop effective anticancer drugs. There is an increase in number of chemotherapy treatments
due to growing number of manifestations causing increasing toxicities of cytotoxic agents. Almost all the
anticancer agents available till date have one or the other side effects. Topoisomerases are the attractive
targets to develop effective anticancer agents. There has been development of many topoisomerase
inhibitors till date and has shown good anticancer activity but their side effects outnumber their
anticancer potential. Hence, there is an urgent need to develop effective therapeutic agents with fewer
side effects. This review deals with design and development aspect of topoisomerase inhibitors as
exciting novel anticancer agents. The emphasis has been laid in particular on the new potential
heterocyles as TOP inhibitors in the field of medicinal chemistry. The review discusses about the
topoisomerase poisons, TOP1 suppressors, TOP inhibitors and Dual TOP 1/2 inhibitors.
Keywords: Anticancer, topoisomerase types and inhibitors, structure activity relationship, topoisomerase inhibitors.
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