Franz Bracher* and Tim Tremmel Pages 92 - 98 ( 7 )
Background: The canthin-4-ones are a small, yet underexplored class of natural products from Apocynaceae plants. Efficient synthetic approaches are required for exploring this class of natural products for drug discovery.Objective: In this review, the synthetic approaches towards these alkaloids, as well as synthetic analogues are summarized comprehensively. Further, the applications of canthin-4-ones as building blocks for the synthesis of alkaloids and other polycyclic compounds of pharmaceutical interest are demonstrated. Conclusion: Meanwhile, efficient and flexible approaches to the canthin-4-one scaffold are available which should foster in-depth investigation of this chemotype for drug development.
Canthin-4-ones, alkaloids, total synthesis, β-carbolines, ring transformation, biological activity.
Department of Pharmacy, Ludwig-Maximilians University, Butenandtstr. 5-13, 81377 Munich, Department of Pharmacy, Center for Drug Research, Ludwig-Maximilians University, Munich