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Acridine-based Anticancer Drugs

  • Chapter
Molecular Aspects of Anticancer Drug-DNA Interactions

Part of the book series: Topics in Molecular and Structural Biology ((TMSB))

Abstract

We have previously (Denny et al., 1983) outlined the considerable importance of acridines in clinical medicine, dating from the early years of the twentieth century, primarily as antibacterial and antimalarial agents. We also noted the changing of this emphasis, with the more recent development of acridine-based compounds as anticancer drugs, e.g. amsacrine (m-AMSA, NSC 249992) (1) and nitracrine (2). This trend has continued since 1983, as can be seen in this chapter. The primary mechanism of action of amsacrine, inhibition of the religation reaction of DNA topoisomerase II, has been elucidated and shown to be common to many DNA-intercalating agents, as described elsewhere in this volume. In addition to its clinical antitumour properties, amsacrine has considerable importance as a biochemical reagent for studying topoisomerase II. Further work on the acridines has uncovered a number of derivatives with varied and promising activities. An analogue of amsacrine (CI-921; NSC 343499) (3) has reached clinical trial, while another acridine derivative (acridinecarboxamide; DACA, NSC 601136) (4) is about to begin trials. The nitroacridines (e.g. nitracrine) have been shown to have an important new type of biological activity (hypoxia-selective cytotoxicity).

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Authors
  1. William A. Denny
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  2. Bruce C. Baguley
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Editor information

Editors and Affiliations

  1. Institute of Cancer Research, Sutton, Surrey, UK

    Stephen Neidle

  2. Dept of Pharmacology, University of Cambridge, UK

    Michael Waring

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Denny, W.A., Baguley, B.C. (1994). Acridine-based Anticancer Drugs. In: Neidle, S., Waring, M. (eds) Molecular Aspects of Anticancer Drug-DNA Interactions. Topics in Molecular and Structural Biology. Palgrave, London. https://doi.org/10.1007/978-1-349-13330-7_7

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  • DOI: https://doi.org/10.1007/978-1-349-13330-7_7

  • Publisher Name: Palgrave, London

  • Print ISBN: 978-1-349-13332-1

  • Online ISBN: 978-1-349-13330-7

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