Title:Therapeutic Potential of Indole Derivatives as Anti-HIV Agents: A
Mini-review
Volume: 22
Issue: 12
Author(s): Qingtai Chen, Chongchong Wu*, Jinjin Zhu, Enzhong Li and Zhi Xu*
Affiliation:
- Department of Chemical and Petroleum Engineering, University of Calgary, T2N 1N4 Calgary, Alberta, Canada
- Zhumadian Academy of Industry Innovation and Development, Huanghuai University, Zhumadian, 463000, China
Keywords:
Indole, Alkaloids, Hybrid compounds, Dimers, HIV, AIDS, Drug resistance, Structure-activity relationship.
Abstract: Acquired immunodeficiency syndrome (AIDS), caused by the human immunodeficiency
virus (HIV), is one of the leading causes of human deaths. The advent of different anti-HIV drugs has
turned AIDS/HIV from a deadly infection to chronic and manageable disease. However, the development
of multidrug-resistant viruses, along with the severe side effects of anti-HIV agents, has compromised
their efficacy and limited the treatment options. Indoles, the most common frameworks in
the bioactive molecules, represent attractive scaffolds for designing and developing novel drugs. Indole
derivatives are potent inhibitors of HIV enzymes such as reverse transcriptase, integrase, and
protease. Furthermore, some indole-based agents, like delavirdine, have already been applied in clinics
or are under clinical evaluations for the treatment of AIDS/HIV, revealing that indole moiety is a
useful template for the development of anti-HIV agents. This review focuses on the recent advancement
in indole derivatives, including indole alkaloids, hybrids, and dimers with anti-HIV potential,
covering articles published between 2010 and 2020. The chemical structures, structure-activity relationship,
and mechanisms of action are also discussed.