Anti-trypanosomal activities of DNA topoisomerase inhibitors

Deterding, Alexander, Dungey, Fiona A., Thompson, Katy-Anne and Steverding, Dietmar (2005) Anti-trypanosomal activities of DNA topoisomerase inhibitors. Acta Tropica, 93 (3). pp. 311-316.

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Abstract

Only four drugs are available for chemotherapy of human African sleeping sickness with undesirable toxic side effects. The development of new anti-trypanosomal drugs is, therefore, urgently required. In this study, 15 DNA topoisomerase inhibitors, including approved anti-cancer drugs, were tested for in vitro activity against bloodstream forms of Trypanosoma brucei and human leukaemia HL-60 cells. All compounds exhibited anti-trypanosomal activity, with ED50 values ranging between 3 nM and 30 microM, and MIC values between 100 nM and >100 microM. The trypanocidal activities of the most effective DNA topoisomerase inhibitors, aclarubicin, doxorubicin and mitoxantrone, were comparable with those of commercial anti-trypanosomal drugs. These data support the use of DNA topoisomerase inhibitors as lead compounds for anti-trypanosomal drug development.

Item Type: Article
Faculty \ School: Faculty of Medicine and Health Sciences > Norwich Medical School
Depositing User: EPrints Services
Date Deposited: 25 Nov 2010 11:09
Last Modified: 21 Apr 2020 20:01
URI: https://ueaeprints.uea.ac.uk/id/eprint/12513
DOI: 10.1016/j.actatropica.2005.01.005

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