Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors.
Publication
, Journal Article
Dang, Z; Lai, W; Qian, K; Ho, P; Lee, K-H; Chen, C-H; Huang, L
Published in: J Med Chem
December 10, 2009
We previously reported that [[N-[3beta-hydroxyllup-20(29)-en-28-oyl]-7-aminoheptyl]carbamoyl]methane (A43D, 4) was a potent HIV-1 entry inhibitor. However, 4 was inactive against HIV-2 virus, suggesting the structural requirements for targeting these two retroviruses are different. In this study, a series of new betulinic acid derivatives were synthesized, and some of them displayed selective anti-HIV-2 activity at nanomolar concentrations. In comparison to compounds with anti-HIV-1 activity, a shorter C-28 side chain is required for optimal anti-HIV-2 activity.
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Published In
J Med Chem
DOI
EISSN
1520-4804
Publication Date
December 10, 2009
Volume
52
Issue
23
Start / End Page
7887 / 7891
Location
United States
Related Subject Headings
- Triterpenes
- Pentacyclic Triterpenes
- Medicinal & Biomolecular Chemistry
- Inhibitory Concentration 50
- Humans
- HIV-2
- HIV-1
- Dose-Response Relationship, Drug
- Cell Line
- Betulinic Acid
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MLA
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Dang, Z., Lai, W., Qian, K., Ho, P., Lee, K.-H., Chen, C.-H., & Huang, L. (2009). Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors. J Med Chem, 52(23), 7887–7891. https://doi.org/10.1021/jm9004253
Dang, Zhao, Weihong Lai, Keduo Qian, Phong Ho, Kuo-Hsiung Lee, Chin-Ho Chen, and Li Huang. “Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors.” J Med Chem 52, no. 23 (December 10, 2009): 7887–91. https://doi.org/10.1021/jm9004253.
Dang Z, Lai W, Qian K, Ho P, Lee K-H, Chen C-H, et al. Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors. J Med Chem. 2009 Dec 10;52(23):7887–91.
Dang, Zhao, et al. “Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors.” J Med Chem, vol. 52, no. 23, Dec. 2009, pp. 7887–91. Pubmed, doi:10.1021/jm9004253.
Dang Z, Lai W, Qian K, Ho P, Lee K-H, Chen C-H, Huang L. Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors. J Med Chem. 2009 Dec 10;52(23):7887–7891.
Published In
J Med Chem
DOI
EISSN
1520-4804
Publication Date
December 10, 2009
Volume
52
Issue
23
Start / End Page
7887 / 7891
Location
United States
Related Subject Headings
- Triterpenes
- Pentacyclic Triterpenes
- Medicinal & Biomolecular Chemistry
- Inhibitory Concentration 50
- Humans
- HIV-2
- HIV-1
- Dose-Response Relationship, Drug
- Cell Line
- Betulinic Acid