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52 p, 1.9 MB Design, synthesis, structure-activity relationships and X-ray structural studies of novel 1-oxopyrimido[4,5-c]quinoline-2-acetic acid derivatives as selective and potent inhibitors of human aldose reductase / Crespo, Isidro (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) ; Giménez-Dejoz, Joan (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) ; Porté, Sergio (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) ; Cousido-Siah, Alexandra (Institut de Génétique et de Biologie Moléculaire et Cellulaire, France) ; Mitschler, André (Institut de Génétique et de Biologie Moléculaire et Cellulaire, France) ; Podjarny, Alberto (Institut de Génétique et de Biologie Moléculaire et Cellulaire, France) ; Pratsinis, Harris (Institute of Biosciences and Applications, National Centre of Scientific Research "Demokritos", Athens, Greece) ; Kletsas, Dimitris (Institute of Biosciences and Applications, National Centre of Scientific Research "Demokritos", Athens, Greece) ; Parés i Casasampera, Xavier (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular) ; Ruiz, Francesc Xavier (Institut de Génétique et de Biologie Moléculaire et Cellulaire, France) ; Metwally, Kamel (Zagazig University, Egypt) ; Farrés, Jaume (Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular)
Human aldose reductase (AKR1B1, AR) is a key enzyme of the polyol pathway, catalyzing the reduction of glucose to sorbitol at high glucose concentrations, as those found in diabetic condition. Indeed, AKR1B1 overexpression is related to diabetes secondary complications and, in some cases, with cancer. [...]
2018 - 10.1016/j.ejmech.2018.04.015
European Journal of Medicinal Chemistry, Vol. 152 (2018) , p. 160-174  

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