Title:Recent Progress of Bioactivities, Mechanisms of Action, Total Synthesis,
Structural Modifications and Structure-activity Relationships of Indole
Derivatives: A Review
Volume: 22
Issue: 21
Author(s): Tianze Li and Hui Xu*
Affiliation:
- College of Plant Protection, Northwest A&F University, Yangling 712100, Shaanxi Province, P.R. China
- School of Marine Sciences, Ningbo University, Ningbo 315211, Zhejiang Province, P.R. China
Keywords:
Indole, indole derivatives, biological activity, mechanism of action, total synthesis, structural modification, structural- activity relationship.
Abstract: Indole (2,3-benzopyrrole) containing a pyrrolyl ring possesses the characteristic of electron-
rich aromatic compounds. Indole occurs in the oil of jasmine and cloves and coal tar. Additionally,
it is also present as a putrefaction product from animals' intestines. Notably, indole and its derivatives
exhibit a wide range of biological properties, such as anti-Alzheimer’s disease, anti-cancer, antibacterial,
anti-inflammatory, anti-human immunodeficiency virus (HIV), anti-diabetic, antituberculosis,
anti-oxidant, anti-coronavirus, and antifungal activities. In this mini-review, recent advances
in biological activities, mechanisms of action, total synthesis, structural modifications, and
structure-activity relationships of indole and its derivatives from 2018 to 2020 are described. We hope
the present paper can pave the way for future design, development, and application of indole derivatives
as potent drugs.