Diverse pharmacological activities of β-carbolines: Substitution patterns, SARs and mechanisms of action

Abstract

β-Carbolines, a class of indole-containing heterocyclic alkaloids, are widely distributed in nature and possess diverse bioactivities, making them promising drug candidates against a wide range of diseases. The remarkable medicinal potential of β-carbolines has spurred the pharmaceutical research community to study their derivatives extensively. This review updates the development of β-carboline derivatives in recent years (2015–2024), particularly with a focus on their anticancer, antiparasitic, antimicrobial, antiviral, and neuroprotective properties, based on the modification approaches such as substitution on indole N (ring B), pyridine or its reduced forms (ring C), and dimerization of β-carbolines. Moreover, the mechanisms of action and structure-activity relationships of these β-carboline derivatives are highlighted to offer valuable insights on the design and development of new β-carbolines with better pharmacological activities.