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Cancer is a leading cause of mortality worldwide, being responsible for millions of deaths annually. Therefore, novel cancer chemotherapeutic agents are urgently needed to combat this devastating disease. β - Carboline alkaloids are an important class of natural products and medicinal molecules, which exert their anticancer activities through diverse mechanisms. In this review, we cover recent natural and synthetic β - carbolines with anticancer activity that have been reported in the literature (2010-July 2014), focusing on their chemical structures, anticancer properties, structure-activity relationships, and mechanisms of action.