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

Eur J Med Chem

Key Laboratory for Green Chemical Process of Ministry of Education, Hubei Key Laboratory of Novel Reactor and Green Chemical Technology, Hubei Engineering Research Center for Advanced Fine Chemicals, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, 206 1st Rd Optics Valley

Published: April 2025


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Article 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.

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http://dx.doi.org/10.1016/j.ejmech.2025.117350DOI Listing

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