Anti-trypanosomal activities of DNA topoisomerase inhibitors

Alexander Deterding, Fiona A. Dungey, Katy-Anne Thompson, Dietmar Steverding

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47 Citations (Scopus)


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.
Original languageEnglish
Pages (from-to)311-316
Number of pages6
JournalActa Tropica
Issue number3
Publication statusPublished - 2005

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