Cancer, an uncontrolled and rapid proliferation of abnormal cells, has become one of the leading cause of death worldwide. The development of resistance among the numerous drugs in clinical use has provided strong impetus for the identification and development of novel cancer therapeutics. β-carbolines constitute an important class of pharmacologically active scaffolds known to exert their anticancer activities via diverse mechanisms. The purpose of present review article is to update the readers on the current developments in β-carbolines with an emphasis on synthetic strategies, structure-activity relationships, mechanism of action and in vivo studies wherever possible.