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

Authors
  • Jin, Tian1
  • Zhai, Jing2
  • Liu, Xiao1
  • Yue, Yan1
  • Huang, Maolin1
  • Li, Zonghe1
  • Ni, Caixia1
  • Deng, Qishan1
  • Sang, Yankui1
  • Yao, Zhongwei1
  • Zhang, Hong1
  • Hu, Xiaopeng2
  • Zheng, Zhe-Bin1
  • 1 Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Insititute of Antibiotics, Chengdu University.
  • 2 School of Pharmaceutical Sciences & Centre for Cellular and Structural Biology of Sun Yet-Sen University.
Type
Published Article
Journal
Chemical and Pharmaceutical Bulletin
Publisher
Pharmaceutical Society of Japan
Publication Date
May 01, 2017
Volume
65
Issue
5
Pages
455–460
Identifiers
DOI: 10.1248/cpb.c16-00800
PMID: 28320998
Source
Medline
Keywords
License
Unknown

Abstract

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.

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