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  • Synthesis of novel nitroxoline analogs with potent cathepsin B exopeptidase inhibitory activity [Elektronski vir]
    Van de Walle, Tim ...
    Nitroxoline, a well-known antimicrobial agent, has been identified in several independent studies, and on different molecular targets, as a promising candidate to be repurposed for cancer treatment. ... One specific target of interest concerns cathepsin B, a lysosomal peptidase involved in the degradation of the extracellular matrix (ECM), leading to tumor invasion, metastasis and angiogenesis. However, dedicated optimization of the nitroxoline core is needed to actually deliver a nitroxoline-based antitumor drug candidate. Within that context, 34 novel nitroxoline analogs were synthesized and evaluated for their relative cathepsin B inhibitory activity, their antiproliferative properties and their antimicrobial activity. More than twenty analogs were shown to exert a similar or even slightly higher cathepsin B inhibitory activity compared to nitroxoline. The implemented modifications of the nitroxoline scaffold and the resulting SAR information can form an eligible basis for further optimization toward more potent cathepsin B inhibitors in the quest for a clinical nitroxoline-based antitumor agent.
    Vir: ChemMedChem. - ISSN 1860-7187 (Vol. 15, iss. 24, 2020, str. 2477-2490)
    Vrsta gradiva - e-članek
    Leto - 2020
    Jezik - angleški
    COBISS.SI-ID - 24827139

    Povezava(-e):

    https://chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/cmdc.202000402
    DOI

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