Anti-AIDS agents 88. Anti-HIV conjugates of betulin and betulinic acid with AZT prepared via click chemistry.
Publication
, Journal Article
Bori, ID; Hung, H-Y; Qian, K; Chen, C-H; Morris-Natschke, SL; Lee, K-H
Published in: Tetrahedron Lett
April 11, 2012
In the present study, a new strategy to link AZT with betulin/betulinic acid (BA) by click chemistry was designed and achieved. This conjugation via a triazole linkage offers a new direction for modification of anti-HIV triterpenes. Click chemistry provides an easy and productive way for linking two molecules, even when one of them is a large natural product. Among the newly synthesized conjugates, compounds 15 and 16 showed potent anti-HIV activity with EC(50) values of 0.067 and 0.10 µM, respectively, which are comparable to that of AZT (EC(50): 0.10 µM) in the same assay.
Duke Scholars
Published In
Tetrahedron Lett
DOI
ISSN
0040-4039
Publication Date
April 11, 2012
Volume
53
Issue
15
Start / End Page
1987 / 1989
Location
England
Related Subject Headings
- Organic Chemistry
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry
- 3101 Biochemistry and cell biology
- 0305 Organic Chemistry
- 0304 Medicinal and Biomolecular Chemistry
Citation
APA
Chicago
ICMJE
MLA
NLM
Bori, I. D., Hung, H.-Y., Qian, K., Chen, C.-H., Morris-Natschke, S. L., & Lee, K.-H. (2012). Anti-AIDS agents 88. Anti-HIV conjugates of betulin and betulinic acid with AZT prepared via click chemistry. Tetrahedron Lett, 53(15), 1987–1989. https://doi.org/10.1016/j.tetlet.2012.02.022
Bori, Ibrahim D., Hsin-Yi Hung, Keduo Qian, Chin-Ho Chen, Susan L. Morris-Natschke, and Kuo-Hsiung Lee. “Anti-AIDS agents 88. Anti-HIV conjugates of betulin and betulinic acid with AZT prepared via click chemistry.” Tetrahedron Lett 53, no. 15 (April 11, 2012): 1987–89. https://doi.org/10.1016/j.tetlet.2012.02.022.
Bori ID, Hung H-Y, Qian K, Chen C-H, Morris-Natschke SL, Lee K-H. Anti-AIDS agents 88. Anti-HIV conjugates of betulin and betulinic acid with AZT prepared via click chemistry. Tetrahedron Lett. 2012 Apr 11;53(15):1987–9.
Bori, Ibrahim D., et al. “Anti-AIDS agents 88. Anti-HIV conjugates of betulin and betulinic acid with AZT prepared via click chemistry.” Tetrahedron Lett, vol. 53, no. 15, Apr. 2012, pp. 1987–89. Pubmed, doi:10.1016/j.tetlet.2012.02.022.
Bori ID, Hung H-Y, Qian K, Chen C-H, Morris-Natschke SL, Lee K-H. Anti-AIDS agents 88. Anti-HIV conjugates of betulin and betulinic acid with AZT prepared via click chemistry. Tetrahedron Lett. 2012 Apr 11;53(15):1987–1989.
Published In
Tetrahedron Lett
DOI
ISSN
0040-4039
Publication Date
April 11, 2012
Volume
53
Issue
15
Start / End Page
1987 / 1989
Location
England
Related Subject Headings
- Organic Chemistry
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry
- 3101 Biochemistry and cell biology
- 0305 Organic Chemistry
- 0304 Medicinal and Biomolecular Chemistry