The invention relates to a use of ugonin compounds in manufacturing drugs for treating skin cancer by applying an effective does of the ugonin compounds to skin for inducing cell cycle arrest, regulating expression of cell cycle-related genes or proteins, stimulating expression of apoptosis-related genes or proteins, and decreasing migration and invasion of cancer cells. Accordingly, the ugonin compounds can be further utilized in manufacturing pharmaceutical compositions for treating skin cancer or slowing down development of skin cancer, so as to effectively inhibit proliferation, migration and invasion of skin cancer cells.