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Synthesis and proteasome inhibition of glycyrrhetinic acid derivatives.

Publication ,  Journal Article
Huang, L; Yu, D; Ho, P; Qian, K; Lee, K-H; Chen, C-H
Published in: Bioorg Med Chem
July 15, 2008

This study discovered that glycyrrhetinic acid inhibited the human 20S proteasome at 22.3microM. Esterification of the C-3 hydroxyl group on glycyrrhetinic acid with various carboxylic acid reagents yielded a series of analogs with marked improved potency. Among the derivatives, glycyrrhetinic acid 3-O-isophthalate (17) was the most potent compound with IC(50) of 0.22microM, which was approximately 100-fold more potent than glycyrrhetinic acid.

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Published In

Bioorg Med Chem

DOI

EISSN

1464-3391

Publication Date

July 15, 2008

Volume

16

Issue

14

Start / End Page

6696 / 6701

Location

England

Related Subject Headings

  • Structure-Activity Relationship
  • Proteasome Inhibitors
  • Protease Inhibitors
  • Medicinal & Biomolecular Chemistry
  • Humans
  • Glycyrrhetinic Acid
  • Esterification
  • 3405 Organic chemistry
  • 3404 Medicinal and biomolecular chemistry
  • 3101 Biochemistry and cell biology
 

Citation

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Huang, L., Yu, D., Ho, P., Qian, K., Lee, K.-H., & Chen, C.-H. (2008). Synthesis and proteasome inhibition of glycyrrhetinic acid derivatives. Bioorg Med Chem, 16(14), 6696–6701. https://doi.org/10.1016/j.bmc.2008.05.078
Huang, Li, Donglei Yu, Phong Ho, Keduo Qian, Kuo-Hsiung Lee, and Chin-Ho Chen. “Synthesis and proteasome inhibition of glycyrrhetinic acid derivatives.Bioorg Med Chem 16, no. 14 (July 15, 2008): 6696–6701. https://doi.org/10.1016/j.bmc.2008.05.078.
Huang L, Yu D, Ho P, Qian K, Lee K-H, Chen C-H. Synthesis and proteasome inhibition of glycyrrhetinic acid derivatives. Bioorg Med Chem. 2008 Jul 15;16(14):6696–701.
Huang, Li, et al. “Synthesis and proteasome inhibition of glycyrrhetinic acid derivatives.Bioorg Med Chem, vol. 16, no. 14, July 2008, pp. 6696–701. Pubmed, doi:10.1016/j.bmc.2008.05.078.
Huang L, Yu D, Ho P, Qian K, Lee K-H, Chen C-H. Synthesis and proteasome inhibition of glycyrrhetinic acid derivatives. Bioorg Med Chem. 2008 Jul 15;16(14):6696–6701.
Journal cover image

Published In

Bioorg Med Chem

DOI

EISSN

1464-3391

Publication Date

July 15, 2008

Volume

16

Issue

14

Start / End Page

6696 / 6701

Location

England

Related Subject Headings

  • Structure-Activity Relationship
  • Proteasome Inhibitors
  • Protease Inhibitors
  • Medicinal & Biomolecular Chemistry
  • Humans
  • Glycyrrhetinic Acid
  • Esterification
  • 3405 Organic chemistry
  • 3404 Medicinal and biomolecular chemistry
  • 3101 Biochemistry and cell biology