DNA intercalators in cancer therapy: organic and inorganic drugs and their spectroscopic tools of analysis

N.J. Wheate, J.G. Collins, S. Kemp, J.R. Aldrich-Wright, C.R. Brodie

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Since the discovery of the DNA intercalation process by Lerman in 1961 thousands of organic, inorganic octahedral (particularly ruthenium(II) and rhodium(III)) and square-planar (particularly platinum(II)) compounds have been developed as potential anticancer agents and diagnostic agents. The design and synthesis of new drugs is focused on bis-intercalators which have two intercalating groups linked via a variety of ligands, and synergistic drugs, which combine the anticancer properties of intercalation with other functionalities, such as covalent binding or boron-cages (for radiation therapy). Advances in spectroscopic techniques mean that the process of DNA intercalation can be examined in far greater detail than ever before, yielding important information on structure-activity relationships. In this review we examine the history and development of DNA intercalators as anticancer agents and advances in the analysis of DNA-drug interactions.
Original languageEnglish
Pages (from-to)627-648
Number of pages21
JournalMini-Reviews in Medicinal Chemistry
Issue number6
Publication statusPublished - Jun 2007


  • DNA intercalation
  • bis-intercalation
  • synergistic
  • anticancer
  • cytotoxicity
  • spectrometry
  • review

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