Abstract

DNA intercalating and minor groove binding compounds are new weapons in the battle against malignant diseases. These antineoplastic agents target the DNA molecule and interfere with the cell cycle leading to rapidly proliferating cell death. They are mainly derivates of a naturally occurring organic compound derived from a microorganism or plant. Intercalators usually act as topoisomerase I and/or II poisons, while the mechanisms of DNA minor groove binders are a combination of several steps including topoisomerase poisoning. This paper gives an overview of some of the developed DNA intercalating and minor groove binding compounds, as well as an explanation of their chemical structures, origins, and application in chemotherapy.

Highlights

  • Intercalators usually act as topoisomerase I and/or II poisons, while the mechanisms of DNA minor groove binders are a combination of several steps including topoisomerase poisoning

  • In the last 70 years, more than 175 antitumour drugs have been produced and commercialised, 65 % of which were derived from natural products [4, 5] or were newly-synthesized molecules that contained pharmacophores from natural products [3]

  • The complex created between DNA and a small molecule can modify normal gene expression leading to alterations in the regulation of cell growth [14]

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Summary

Introduction

DNA intercalating and minor groove binding compounds are new weapons in the battle against malignant diseases. Intercalators usually act as topoisomerase I and/or II poisons, while the mechanisms of DNA minor groove binders are a combination of several steps including topoisomerase poisoning. This paper gives an overview of some of the developed DNA intercalating and minor groove binding compounds, as well as an explanation of their chemical structures, origins, and application in chemotherapy.

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