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  • Structure-activity relationships of triazole-benzodioxine inhibitors of cathepsin X
    Pečar Fonović, Urša ...
    Cathepsin X is a cysteine carboxypeptidase that is involved in various physiological and pathological processes. In particular, highly elevated expression and activity of cathepsin X has been ... observed in cancers and neurodegenerative diseases. Previously, we identified compound Z9 (1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-2-((4-isopropyl-4H-1,2,4-triazol-3-yl)thio)ethan-1-one) as a potent and specific reversible cathepsin X inhibitor. Here, we have explored the effects of chemical variations to Z9 of either benzodioxine or triazol moieties, and the importance of the central ketomethylenethio linker. The ketomethylenethio linker was crucial for cathepsin X inhibition, whereas changes of the triazole heterocycle did not alter the inhibitory potencies to a greater extent. Replacement of benzodioxine moiety with substituted benzenes reduced cathepsin X inhibition. Overall, several synthesized compounds showed similar or improved inhibitory potencies against cathepsin X compared to Z9, with IC50 values of 7.1 micorM-13.6 microM. Additionally, 25 inhibited prostate cancer cell migration by 21%, which is under the control of cathepsin X.
    Vir: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 193, 2020, str. 1-17)
    Vrsta gradiva - članek, sestavni del ; neleposlovje za odrasle
    Leto - 2020
    Jezik - angleški
    COBISS.SI-ID - 4896113

    Povezava(-e):

    https://www.sciencedirect.com/science/article/pii/S0223523420301859
    DOI

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