β-Carboline is a crucial compound in medicinal chemistry known for its versatile pharmacological activities. Recent research has focused on hybrid molecules incorporating a β-carboline scaffold linked to other pharmacophore moieties. These hybrid compounds have demonstrated diverse therapeutic properties, including anticancer, antianxiety, antimalarial, antidepressant, anti-inflammatory, antileishmanial, and antioxidant effects. This review highlights studies conducted from 2014 to the present with a particular emphasis on the development of β-carboline hybrid compounds and their derivatives as potent anticancer agents. The structure-activity relationship (SAR) analysis reveals that these hybrids exhibit significant cytotoxicity against various cancer cell lines. This review aims to inspire further research into the novel synthesis and evolution of β-carboline hybrids and their derivatives, potentially leading to new therapeutic advancements.