Design, Synthesis and Biological Evaluation of Potent Human Glyoxalase I Inhibitors

Several glutathione derivatives bearing the S-(N-aryl-N-hydroxycarbamoyl) or S-(C-aryl-N-hydroxycarbamoyl) moieties (10, 10′, 13–15) were synthesized, characterized, and their human glyoxalase I (hGLO1) inhibitory activity was evaluated. Compound 10 was proved to be the effective hGLO1 inhibitor wit...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 2017/05/01, Vol.65(5), pp.455-460
Hauptverfasser:	Jin, Tian, Zhai, Jing, Liu, Xiao, Yue, Yan, Huang, Maolin, Li, Zonghe, Ni, Caixia, Deng, Qishan, Sang, Yankui, Yao, Zhongwei, Zhang, Hong, Hu, Xiaopeng, Zheng, Zhe-Bin
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Aromatic compounds Biological Assay Cell Line, Tumor cell membrane permeability study Drug Design Enzyme Activation - drug effects Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Esters - chemical synthesis Esters - chemistry Esters - pharmacology Glutathione Glutathione - chemical synthesis Glutathione - chemistry Glutathione - pharmacology glyoxalase I inhibitor Humans inhibition constant Inhibitors Lactoylglutathione lyase Lactoylglutathione Lyase - antagonists & inhibitors Mice Models, Biological Molecular Structure NCI-H522 cell line synthesis Tumor Burden - drug effects Xenografts
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