New betulinic acid derivatives as potent proteasome inhibitors.
Publication
, Journal Article
Qian, K; Kim, S-Y; Hung, H-Y; Huang, L; Chen, C-H; Lee, K-H
Published in: Bioorg Med Chem Lett
October 1, 2011
In this study, 22 new betulinic acid (BA) derivatives were synthesized and tested for their inhibition of the chymotrypsin-like activity of 20S proteasome. From the SAR study, we concluded that the C-3 and C-30 positions are the pharmacophores for increasing the proteasome inhibition effects, and larger lipophilic or aromatic side chains are favored at these positions. Among the BA derivatives tested, compounds 13, 20, and 21 showed the best proteasome inhibition activity with IC(50) values of 1.42, 1.56, and 1.80 μM, respectively, which are three to fourfold more potent than the proteasome inhibition controls LLM-F and lactacystin.
Duke Scholars
Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
October 1, 2011
Volume
21
Issue
19
Start / End Page
5944 / 5947
Location
England
Related Subject Headings
- Triterpenes
- Structure-Activity Relationship
- Signal Transduction
- Proteasome Inhibitors
- Pentacyclic Triterpenes
- Neoplasms
- Molecular Targeted Therapy
- Molecular Structure
- Medicinal & Biomolecular Chemistry
- Inflammation
Citation
APA
Chicago
ICMJE
MLA
NLM
Qian, K., Kim, S.-Y., Hung, H.-Y., Huang, L., Chen, C.-H., & Lee, K.-H. (2011). New betulinic acid derivatives as potent proteasome inhibitors. Bioorg Med Chem Lett, 21(19), 5944–5947. https://doi.org/10.1016/j.bmcl.2011.07.072
Qian, Keduo, Sang-Yong Kim, Hsin-Yi Hung, Li Huang, Chin-Ho Chen, and Kuo-Hsiung Lee. “New betulinic acid derivatives as potent proteasome inhibitors.” Bioorg Med Chem Lett 21, no. 19 (October 1, 2011): 5944–47. https://doi.org/10.1016/j.bmcl.2011.07.072.
Qian K, Kim S-Y, Hung H-Y, Huang L, Chen C-H, Lee K-H. New betulinic acid derivatives as potent proteasome inhibitors. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5944–7.
Qian, Keduo, et al. “New betulinic acid derivatives as potent proteasome inhibitors.” Bioorg Med Chem Lett, vol. 21, no. 19, Oct. 2011, pp. 5944–47. Pubmed, doi:10.1016/j.bmcl.2011.07.072.
Qian K, Kim S-Y, Hung H-Y, Huang L, Chen C-H, Lee K-H. New betulinic acid derivatives as potent proteasome inhibitors. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5944–5947.
Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
October 1, 2011
Volume
21
Issue
19
Start / End Page
5944 / 5947
Location
England
Related Subject Headings
- Triterpenes
- Structure-Activity Relationship
- Signal Transduction
- Proteasome Inhibitors
- Pentacyclic Triterpenes
- Neoplasms
- Molecular Targeted Therapy
- Molecular Structure
- Medicinal & Biomolecular Chemistry
- Inflammation