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Their relatively simple structure and ease of modification have drawn lasting interest from medicinal chemists. This review organizes their pharmacological activities according to structural types: simple \u03b2\u2010carbolines, those with substitutions at the C\u20101, N\u20102\/N\u20109 or C\u20103 positions, cyclized derivatives, and bis\u2010\u03b2\u2010carboline dimers. For each type, we discuss reported mechanisms, such as inhibition of CDK4, HDAC, and topoisomerases. The available data point to promising applications in cancer, inflammatory disorders, and infectious diseases. 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