Spirodienone derivatives have unique structural characteristics. Its spiroatoms are quaternary carbons that act as bridges between dienone and four, five, six and even seven heterocycles or carbon rings. The structural unit not only shows unique properties in organic chemistry but also demonstrates a variety of biological activities. Herein, we overviewed the biological activities and the synthesis methods of spirodienone derivatives for the first time, hoping to benefit the development and design based on novel drugs of spirodienone derivatives. The spirodienone derivatives discussed in this review included spirolactam, spirocarbon rings and spiroheterocycles, where 4-or 6-are spirocyclic atoms (Fig. 1).