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Natural products are important sources of therapeutic drugs. However, it is a challenge to simplify the structure of natural products without decreasing the biological activity. Here we provide the first example of the successful simplification of an antifungal natural product. Starting from sampangine, two novel simplified scaffolds with excellent antifungal activity were discovered.

Graphical abstract: The discovery of novel antifungal scaffolds by structural simplification of the natural product sampangine

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