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  • New inhibitors of fungal 17ß-hydroxysteroid dehydrogenase based on the (1,5)-benzodiazepine scaffold
    Živec, Matej, 1979- ...
    The synthesis and activity of a new series of non-steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase are based on a 1,5-benzodiazepine scaffoldare presented. Their inhibitory potential was ... screened against 17beta-hydroxysteroid dehydrogenase from the fungus Cochliobolus luuatus (17beta-HSDcI), a model enzyme of the short-chain dehydrogenasež reductase superfamily. Some of these compounds are potent inhibitors of 17beta-HSDcI activity, with IC50 values in the low micromolar range and represent promisinglead compounds that should be further developed and investigated as inhibitors of human 17beta-HSD isoforms, which are the enzymes associated withthe development of many hormone-dependent and neuronal diseases.
    Vrsta gradiva - članek, sestavni del
    Leto - 2007
    Jezik - angleški
    COBISS.SI-ID - 21592281