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  • Cathepsin B inhibitors : further exploration of the nitroxoline core
    Sosič, Izidor ...
    Human cathepsin B is a cysteine protease with many house-keeping functions, such as intracellular proteolysis within lysosomes. Its increased activity and expression have been strongly associated ... with many pathological processes, including cancers. We present here the design and synthesis of novel derivatives of nitroxoline as inhibitors of cathepsin B. These were prepared either by omitting the pyridine part, or by modifying positions 2, 7, and 8 of nitroxoline. All compounds were evaluated for their ability to inhibit endopeptidase and exopeptidase activities of cathepsin B. For the most promising inhibitors, the ability to reduce extracellular and intracellular collagen IV degradation was determined, followed by their evaluation in cell-based in vitro models of tumor invasion. The presented data show that we have further defined the structural requirements for cathepsin B inhibition by nitroxoline derivatives and provided additional knowledge that could lead to non-peptidic compounds with usefulness against tumor progression.
    Source: Bioorganic & Medicinal Chemistry Letters. - ISSN 0960-894X (Vol. 28, iss. 7, 2018, str. 1239-1247)
    Type of material - article, component part ; adult, serious
    Publish date - 2018
    Language - english
    COBISS.SI-ID - 4477553

    Link(s):

    https://www.sciencedirect.com/science/article/pii/S0960894X18301471
    DOI

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