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

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  • Jin Tian
    Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Insititute of Antibiotics, Chengdu University
  • Zhai Jing
    School of Pharmaceutical Sciences & Centre for Cellular and Structural Biology of Sun Yet-Sen University
  • Liu Xiao
    Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Insititute of Antibiotics, Chengdu University
  • Yue Yan
    Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Insititute of Antibiotics, Chengdu University
  • Huang Maolin
    Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Insititute of Antibiotics, Chengdu University
  • Li Zonghe
    Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Insititute of Antibiotics, Chengdu University
  • Ni Caixia
    Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Insititute of Antibiotics, Chengdu University
  • Deng Qishan
    Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Insititute of Antibiotics, Chengdu University
  • Sang Yankui
    Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Insititute of Antibiotics, Chengdu University
  • Yao Zhongwei
    Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Insititute of Antibiotics, Chengdu University
  • Zhang Hong
    Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Insititute of Antibiotics, Chengdu University
  • Hu Xiaopeng
    School of Pharmaceutical Sciences & Centre for Cellular and Structural Biology of Sun Yet-Sen University
  • Zheng Zhe-Bin
    Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Insititute of Antibiotics, Chengdu University

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<p>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 with a Ki value of 1.0 nM and the inhibition effect of compound 10 on hGLO1 was nearly ten-fold higher than that of the strongest inhibitor 2 (Ki=10.0 nM) which has been reported in the field of glutathione-type hGLO1 inhibitors. Its diethyl ester prodrug 10′ was able to penetrate cell membrane and had good inhibitory effect on the growth of NCI-H522 cell xenograft tumor model.</p>

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