Since the first reported synthesis of an α-carboline almost a century ago, there has been a steady interest in the development of strategies towards this unique heterocyclic motif. This interest can mainly be attributed to a range of biological activity displayed by the α-carboline natural products including cytotoxicity, anticancer properties or CNS activity. Numerous studies have led to the development of a number of alternative methods to prepare simple α-carbolines as well as a range of synthetic α-carboline derived compounds.
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