Conjugates of betulin derivatives with AZT as potent anti-HIV agents.
Publication
, Journal Article
Xiong, J; Kashiwada, Y; Chen, C-H; Qian, K; Morris-Natschke, SL; Lee, K-H; Takaishi, Y
Published in: Bioorg Med Chem
September 1, 2010
Fourteen novel conjugates of 3,28-di-O-acylbetulins with AZT were prepared as anti-HIV agents, based on our previously reported potent anti-HIV triterpene leads, including 3-O-acyl and 3,28-di-O-acylbetulins. Nine of the conjugates (49-53, 55, 56, 59, and 60) exhibited potent anti-HIV activity at the submicromolar level, with EC(50) values ranging from 0.040 to 0.098muM in HIV-1(NL4-3) infected MT-4 cells. These compounds were equipotent or more potent than 3-O-(3',3'-dimethylsuccinyl)betulinic acid (2), which is currently in Phase IIb anti-AIDS clinical trial.
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Published In
Bioorg Med Chem
DOI
EISSN
1464-3391
Publication Date
September 1, 2010
Volume
18
Issue
17
Start / End Page
6451 / 6469
Location
England
Related Subject Headings
- Zidovudine
- Triterpenes
- Pentacyclic Triterpenes
- Medicinal & Biomolecular Chemistry
- Humans
- HIV-1
- Cell Line
- CD4-Positive T-Lymphocytes
- Betulinic Acid
- Anti-HIV Agents
Citation
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ICMJE
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Xiong, J., Kashiwada, Y., Chen, C.-H., Qian, K., Morris-Natschke, S. L., Lee, K.-H., & Takaishi, Y. (2010). Conjugates of betulin derivatives with AZT as potent anti-HIV agents. Bioorg Med Chem, 18(17), 6451–6469. https://doi.org/10.1016/j.bmc.2010.06.092
Xiong, Juan, Yoshiki Kashiwada, Chin-Ho Chen, Keduo Qian, Susan L. Morris-Natschke, Kuo-Hsiung Lee, and Yoshihisa Takaishi. “Conjugates of betulin derivatives with AZT as potent anti-HIV agents.” Bioorg Med Chem 18, no. 17 (September 1, 2010): 6451–69. https://doi.org/10.1016/j.bmc.2010.06.092.
Xiong J, Kashiwada Y, Chen C-H, Qian K, Morris-Natschke SL, Lee K-H, et al. Conjugates of betulin derivatives with AZT as potent anti-HIV agents. Bioorg Med Chem. 2010 Sep 1;18(17):6451–69.
Xiong, Juan, et al. “Conjugates of betulin derivatives with AZT as potent anti-HIV agents.” Bioorg Med Chem, vol. 18, no. 17, Sept. 2010, pp. 6451–69. Pubmed, doi:10.1016/j.bmc.2010.06.092.
Xiong J, Kashiwada Y, Chen C-H, Qian K, Morris-Natschke SL, Lee K-H, Takaishi Y. Conjugates of betulin derivatives with AZT as potent anti-HIV agents. Bioorg Med Chem. 2010 Sep 1;18(17):6451–6469.
Published In
Bioorg Med Chem
DOI
EISSN
1464-3391
Publication Date
September 1, 2010
Volume
18
Issue
17
Start / End Page
6451 / 6469
Location
England
Related Subject Headings
- Zidovudine
- Triterpenes
- Pentacyclic Triterpenes
- Medicinal & Biomolecular Chemistry
- Humans
- HIV-1
- Cell Line
- CD4-Positive T-Lymphocytes
- Betulinic Acid
- Anti-HIV Agents