Mini-Reviews in Medicinal Chemistry


DNA Intercalators in Cancer Therapy: Organic and Inorganic Drugs and Their Spectroscopic Tools of Analysis

Author(s): Nial J. Wheate, Craig R. Brodie, J. Grant Collins, Sharon Kemp and Janice R. Aldrich-Wright

Affiliation: School of Biomedical and Health Sciences, University of Western Sydney, Locked Bag 1797, Penrith South DC, NSW 1797, Australia.


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 bisintercalators 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.

Keywords: DNA intercalation, bis-intercalation, synergistic, anticancer, cytotoxicity, spectrometry, review

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Article Details

Page: [627 - 648]
Pages: 22
DOI: 10.2174/138955707780859413
Price: $58