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Anticancer agents and antitrypanosomiasis activity in mice.

K E Kinnamon, E A Steck, D S Rane

    Journal of the National Cancer Institute
    |February 1, 1980
    PubMed
    Summary

    Researchers screened 303 compounds for anticancer and anti-parasitic activity. A significant percentage of anticancer compounds also showed efficacy against Trypanosoma rhodesiense infections in mice.

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    Area of Science:

    • Medicinal Chemistry
    • Parasitology
    • Pharmacology

    Background:

    • The National Cancer Institute's Drug Synthesis and Chemistry Branch provided 303 compounds for evaluation.
    • These compounds were initially screened for anticancer properties, with 66 identified as active and 237 as inactive.

    Purpose of the Study:

    • To assess the antitrypanosomiasis activity of compounds with known anticancer properties.
    • To identify potential drug candidates with dual anticancer and anti-parasitic efficacy.

    Main Methods:

    • A total of 303 compounds were tested against Trypanosoma rhodesiense infections in ICR/Ha Swiss mice.
    • Compounds were evaluated based on their activity against both cancer and trypanosomiasis.

    Main Results:

    • Twenty-five of the 303 compounds exhibited activity against Trypanosoma rhodesiense.
    • Fifteen of these 25 compounds also possessed anticancer properties.
    • Anticancer compounds demonstrated a 22.7% success rate in exhibiting antitrypanosomiasis activity, compared to 6% for compounds selected by other methods.

    Conclusions:

    • A notable proportion of anticancer compounds also possess antitrypanosomiasis activity.
    • This suggests a potential for developing dual-acting agents for cancer and parasitic diseases.
    • The findings highlight a promising strategy for drug discovery by screening anticancer libraries for antiparasitic potential.

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