β-Carbolines as potential anticancer agents

β-Carbolines are indole alkaloids having a tricyclic pyrido[3,4-b]indole ring in their structure. Since the isolation of first β-carboline from Peganum harmala in 1841, the isolation and synthesis of various β-carboline derivatives surged in the following centuries. β-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 β-carboline containing molecules, its derivatives and congeners. [Display omitted] •The natural sources (both plant and marine) along with the synthetic strategies of various functionalized β-carbolines have been discussed.•The discussion is further elaborated to the anticancer activities of all the synthetic as well as natural β-carboline derivatives.•The compounds are classified on the basis of their mechanism of action and potent compound from each class has been discussed.