β-Carbolines as potential anticancer agents

beta-Carbolines are indole alkaloids having a tricyclic pyrido[3,4-b]indole ring in their structure. Since the isolation of first beta-carboline from Peganum harmala in 1841, the isolation and synthesis of various beta-carboline derivatives surged in the following centuries. beta-Carboline derivatives due to their widespread availability from natural sources, structural flexibility, quick reactivity and interaction with varied anticancer targets such as DNA (intercalation, groove binding, etc.), enzymes (GPX4, topoisomerases, kinases, etc.) and proteins (tubulin, ABCG2/BRCP1, etc.) have established themselves as promising lead compounds for the synthesis of various anticancer active agents. The current review covers the synthesis and isolation, anticancer activity, mechanism of action and SAR of various beta-carboline containing molecules, its derivatives and congeners. (C) 2021 Elsevier Masson SAS. All rights reserved.