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  • An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics

    Author(s)
    Scott, Fraser J
    Khalaf, Abedawn I
    Giordani, Federica
    Wong, Pui Ee
    Duffy, Sandra
    Barrett, Michael
    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 series of 32 structurally diverse MGBs, derived from the natural product distamycin, was evaluated for activity against Trypanosoma brucei brucei. Four compounds have been found to possess significant activity, in the nanomolar range, and represent hits for further optimisation towards novel treatments for Human and Animal African Trypanosomiases. Moreover, SAR indicates that the head group linking moiety is a significant modulator of biological activity.A series of 32 structurally diverse MGBs, derived from the natural product distamycin, was evaluated for activity against Trypanosoma brucei brucei. Four compounds have been found to possess significant activity, in the nanomolar range, and represent hits for further optimisation towards novel treatments for Human and Animal African Trypanosomiases. Moreover, SAR indicates that the head group linking moiety is a significant modulator of biological activity.
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    Journal Title
    European Journal of Medicinal Chemistry
    Volume
    116
    DOI
    https://doi.org/10.1016/j.ejmech.2016.03.064
    Subject
    Medicinal and biomolecular chemistry
    Medicinal and biomolecular chemistry not elsewhere classified
    Organic chemistry
    Pharmacology and pharmaceutical sciences
    Publication URI
    http://hdl.handle.net/10072/142114
    Collection
    • Journal articles

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