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In recent years, the use of natural products for drug discovery has declined in favor of combinatorial methods and the rapid generation of large libraries of potential lead compounds. In their Perspective, Paterson and Anderson suggest that it may be time to revisit the prevailing dogma and consider ways in which natural products could continue to inspire the development of new drugs. Natural products offer high potency and selectivity as a result of long evolutionary selection. Taking bioactive natural substances as a starting point, researchers can then use the methods of organic synthesis to design targeted modifications of specific structures to create new therapeutic agents.