کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1367711 | 981645 | 2005 | 6 صفحه PDF | دانلود رایگان |

Nonsteroidal anti-inflammatory drugs (NSAIDs) like indomethacin, flufenamic acid, and related compounds have been recently identified as potent inhibitors of 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-[(2,2-diphenylacetyl)amino]benzoic acid 4 (IC50 = 11 μM) and 3-phenoxybenzoic acid 10 (IC50 = 0.68 μM). These compounds represent promising starting points for the development of new anticancer agents.
New inhibitors of human recombinant AKR1C3 are reported. Some compounds inhibited the enzyme in submicromolar range.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 23, 1 December 2005, Pages 5170–5175