Structure Optimization of Aloperine Derivatives as HIV-1 Entry Inhibitors.
Publication
, Journal Article
Dang, Z; Xie, H; Zhu, L; Zhang, Q; Li, Z; Huang, L; Chen, C-H
Published in: ACS Med Chem Lett
November 9, 2017
As a step toward developing novel anti-HIV agents, we have identified a class of quinolizidines, including aloperine, that inhibit HIV at 1-5 μM by blocking viral entry. In this study, we have optimized the structure of aloperine and derived compounds with markedly improved activity. Our structural optimization has yielded an aloperine derivative 19 with approximately a 15-fold increase in anti-HIV-1 activity. Our mechanism of action study reveals that compound 19 does not inhibit binding of HIV-1 to receptors but arrests the virus from fusion with the membrane. Binding of the compound to HIV-1gp120 might be responsible for its anti-HIV-1 entry activity.
Duke Scholars
Published In
ACS Med Chem Lett
DOI
ISSN
1948-5875
Publication Date
November 9, 2017
Volume
8
Issue
11
Start / End Page
1199 / 1203
Location
United States
Related Subject Headings
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry
- 1115 Pharmacology and Pharmaceutical Sciences
- 0305 Organic Chemistry
- 0304 Medicinal and Biomolecular Chemistry
Citation
APA
Chicago
ICMJE
MLA
NLM
Dang, Z., Xie, H., Zhu, L., Zhang, Q., Li, Z., Huang, L., & Chen, C.-H. (2017). Structure Optimization of Aloperine Derivatives as HIV-1 Entry Inhibitors. ACS Med Chem Lett, 8(11), 1199–1203. https://doi.org/10.1021/acsmedchemlett.7b00376
Dang, Zhao, Hua Xie, Lei Zhu, Qingye Zhang, Zhijun Li, Li Huang, and Chin-Ho Chen. “Structure Optimization of Aloperine Derivatives as HIV-1 Entry Inhibitors.” ACS Med Chem Lett 8, no. 11 (November 9, 2017): 1199–1203. https://doi.org/10.1021/acsmedchemlett.7b00376.
Dang Z, Xie H, Zhu L, Zhang Q, Li Z, Huang L, et al. Structure Optimization of Aloperine Derivatives as HIV-1 Entry Inhibitors. ACS Med Chem Lett. 2017 Nov 9;8(11):1199–203.
Dang, Zhao, et al. “Structure Optimization of Aloperine Derivatives as HIV-1 Entry Inhibitors.” ACS Med Chem Lett, vol. 8, no. 11, Nov. 2017, pp. 1199–203. Pubmed, doi:10.1021/acsmedchemlett.7b00376.
Dang Z, Xie H, Zhu L, Zhang Q, Li Z, Huang L, Chen C-H. Structure Optimization of Aloperine Derivatives as HIV-1 Entry Inhibitors. ACS Med Chem Lett. 2017 Nov 9;8(11):1199–1203.
Published In
ACS Med Chem Lett
DOI
ISSN
1948-5875
Publication Date
November 9, 2017
Volume
8
Issue
11
Start / End Page
1199 / 1203
Location
United States
Related Subject Headings
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry
- 1115 Pharmacology and Pharmaceutical Sciences
- 0305 Organic Chemistry
- 0304 Medicinal and Biomolecular Chemistry