Authors: demeunynck, M.; Charmantray, F.; Martelli, A.

Source: Current Drug Metabolism, Volume 7, Number 17, 1 November 2001 , pp. 1703-1724(22)

Publisher: Bentham Science Publishers

Abstract:

DNA is considered as one of the main targets for anticancer drug design. The planar structure of acridines confers to the molecules the ability to bind DNA by intercalation and therefore to interfere with metabolic processes. A large number of natural alkaloids and synthetic acridine derivatives have been tested as anticancer agents. So far, a few molecules have entered clinical trials and have been approved for chemotherapy. The mechanisms of action are not fully understood. Cytotoxicity may be related to potent enzyme inhibition. Topoisomerase and telomerase activities may be strongly affected by acridines. The affinity of acridines for DNA has also been used to design new active compounds in which a DNA modifying group is tethered to the acridine nucleus. Acridine derivatives display other pharmacological properties such as antibacterial and antimalarial activities. They are also tested for Alzheimer's disease.

Keywords: Acridine Derivatives; Anticancer Chemotherapy; Cytotoxicity; Antibacterial; Antimalarial; Topoisomerase Inhibitors; Bis-acridinecarboxamide analogues; Telomerase Inhibitors; Acridine Antitumour Agents; Acridone Natural Alkaloids

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1381612013397131

Publication date: 2001-11-01

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• Current Pharmaceutical Design publishes timely in-depth reviews covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area. A Guest Editor who is an acknowledged authority in a therapeutic field has solicits for each issue comprehensive and timely reviews from leading researchers in the pharmaceutical industry and academia.
  
  Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.

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