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  • N-Benzoyl anthranilic acid derivatives as selective inhibitors of aldo/keto reductase AKR1C3
    Sinreih, Maša ...
    Human aldo-keto reductases AKR1C1-AKR1C3 are involved in the biosynthesis and inactivation of steroid hormones and prostaglandins and thus represent attractive targets for the development of new ... drugs. We synthesized a series of N-benzoyl anthranilic acid derivatives and tested their inhibitory activityon AKR1C enzymes. Our data show that these derivatives inhibit AKR1C1-AKR1C3 isoforms with low micromolar potency. In addition, five selective inhibitors of AKR1C3 were identified. The most promising inhibitors were compounds 10 and 13, with IC50 values of 0.31 ?M and 0.35 ?M for AKR1C3, respectively.
    Source: Bioorganic & Medicinal Chemistry Letters. - ISSN 0960-894X (Vol. 22, iss. 18, 2012, str. 5948-5951)
    Type of material - article, component part
    Publish date - 2012
    Language - english
    COBISS.SI-ID - 30074841

    Link(s):

    http://www.sciencedirect.com/science/article/pii/S0960894X12009389
    DOI

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