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  • Selective anti-malarial minor groove binders

    Author(s)
    Scott, Fraser J
    Khalaf, Abedawn I
    Duffy, Sandra
    Avery, Vicky M
    Suckling, Colin J
    Griffith University Author(s)
    Duffy, Sandra
    Avery, Vicky M.
    Year published
    2016
    Metadata
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    Abstract
    A set of 31 DNA minor groove binders (MGBs) with diverse structural features relating to both physical chemical properties and DNA binding sequence preference has been evaluated as potential drugs to treat Plasmodium falciparum infections using a chloroquine sensitive strain (3D7) and a chloroquine resistant strain (Dd2) in comparison with human embryonic kidney (HEK) cells as an indicator of mammalian cell toxicity. MGBs with an alkene link between the two N-terminal building blocks were demonstrated to be most active with IC50 values in the range 30–500 nM and therapeutic ratios in the range 10–>500. Many active compounds ...
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    A set of 31 DNA minor groove binders (MGBs) with diverse structural features relating to both physical chemical properties and DNA binding sequence preference has been evaluated as potential drugs to treat Plasmodium falciparum infections using a chloroquine sensitive strain (3D7) and a chloroquine resistant strain (Dd2) in comparison with human embryonic kidney (HEK) cells as an indicator of mammalian cell toxicity. MGBs with an alkene link between the two N-terminal building blocks were demonstrated to be most active with IC50 values in the range 30–500 nM and therapeutic ratios in the range 10–>500. Many active compounds contained a C-alkylthiazole building block. Active compounds with log D7.4 values of approximately 3 or 7 were identified. Importantly the MGBs tested were essentially equally effective against both chloroquine sensitive and resistant strains. The results show that suitably designed MGBs have the potential for development into clinical candidates for antimalarial drugs effective against resistant strains of Plasmodia.
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    Journal Title
    Bioorganic & Medicinal Chemistry Letters
    Volume
    26
    Issue
    14
    DOI
    https://doi.org/10.1016/j.bmcl.2016.05.039
    Subject
    Medicinal and biomolecular chemistry
    Medicinal and biomolecular chemistry not elsewhere classified
    Organic chemistry
    Pharmacology and pharmaceutical sciences
    Publication URI
    http://hdl.handle.net/10072/142110
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    • Journal articles

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