It is widely accepted that a large number of proteins that are responsible for cellular function exist as dimers or need to be activated by dimerization before mediating certain signaling pathways. Simultaneously targeting both monomeric moieties of the dimeric proteins has shown potential in the development of various therapeutic agents. As dimeric molecules might be able to act on both moieties of a dimeric protein, dimeric sesquiterpenoids (DSs), which are generated biogenetically from coupling of two sesquiterpenoid molecules, are in essence potential biologically active molecules, and have attracted in recent years great attention for their peculiar structures and biological activities. In fact, a number of DSs are more potent than their monomeric precursors for some activities such as anti-inflammatory, anti-tumor, immunosuppressive, potassium channel blocking, antimalarial, anti-virus, and neurotrophic activities.The complex and diversified structures of DSs also attracted attention of chemists in their isolation, structural elucidation, and synthetic construction.In the contribution, a general view of the classification and distribution of DSs will be provided. Strategies for the structural elucidation of DSs and their analogues is presented. Chemical strategies for the convergence of the two sesquiterpenoid units is reviewed. Biological activities are discussed under each type of activity.
Keywords: Compound disesquiterpenoids; Dimeric aza-sesquiterpenoids; Dimeric sesquiterpenoids; Disesquiterpenoids; Nuphar alkaloids; Pseudo-disesquiterpenoids.