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  • Nonsteroidal anti-inflammatory drugs and their analogues as inhibitors of aldo-keto reductase AKR1C3: new lead compounds for the development of anticancer agents
    Gobec, Stanislav, 1970- ; Brožič, Petra ; Lanišnik-Rižner, Tea
    Nonsteroidal anti-inflammatory drugs (NSAIDs) like indomethacin, flufenamic acid, and related compounds have been recently identified as potent inhibitorsof AKR1C3. We report that some other NSAIDs ... (diclofenac and naproxen) also inhibit AKR1C3, with the IC50 values in the low micromolar range. In order to obtain more information about the structure-activity relationship and to identify new leads, a series of compounds designed on the basis of NSAIDs were synthesized and screened on AKR1C3. The most active compounds were 2-š(2,2-diphenylacetyl)aminođbenzoic acid 4 (IC50 = 11 lM) and 3-phenoxybenzoic acid 10 (IC50 = 0.68 lM). These compounds represent promisingstarting points for the development of new anticancer agents.
    Vir: Bioorganic & Medicinal Chemistry Letters. - ISSN 0960-894X (Vol. 15, no. 23, 2005, str. 5170-5175)
    Vrsta gradiva - članek, sestavni del
    Leto - 2005
    Jezik - angleški
    COBISS.SI-ID - 1813873