The invention belongs to the technical field of medicine, and relates to a series of perilla alcohol derivatives disclosed as Formula I, and preparation and application thereof. The invention also relates to pharmaceutically acceptable salts and solvates of the perilla alcohol derivatives, and a pharmaceutical composition containing the perilla alcohol derivatives or pharmaceutically acceptable salts thereof as active components, which can be used for treating cancers. The perilla alcohol derivatives and pharmaceutical salts thereof have favorable anticancer activity. The preparation method is simple and feasible, and is easy to operate.