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.
Duke Scholars
Altmetric Attention Stats
Dimensions Citation Stats
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
APA
Chicago
ICMJE
MLA
NLM
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.
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