Synthesis and structure–activity relationships for 1-(4-(piperidin-1-ylsulfonyl) phenyl) pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase …

…, S Silva, LJM Rigoreau, E Trivier, T Raynham…

Index: Heinrich, Daniel M.; Flanagan, Jack U.; Jamieson, Stephen M.F.; Silva, Shevan; Rigoreau, Laurent J.M.; Trivier, Elisabeth; Raynham, Tony; Turnbull, Andrew P.; Denny, William A. European Journal of Medicinal Chemistry, 2013 , vol. 62, p. 738 - 744

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Citation Number: 18

Abstract

High expression of the aldo-keto reductase enzyme AKR1C3 in the human prostate and breast has implicated it in the development and progression of leukemias and of prostate and breast cancers. Inhibitors are thus of interest as potential drugs. Most inhibitors of AKR1C3 are carboxylic acids, whose transport into cells is likely dominated by carrier- mediated processes. We describe here a series of (piperidinosulfonamidophenyl) ...