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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Review Article

Discovery and Development of Topoisomerase Inhibitors as Anticancer Agents

Author(s): Muthu K. Kathiravan, Anuj N. Kale and Shrikant Nilewar

Volume 16, Issue 15, 2016

Page: [1219 - 1229] Pages: 11

DOI: 10.2174/1389557516666160822110819

Price: $65


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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