In the course of a screening program aimed at cell adhesive inhibitors of microbial origin for metastasis suppression,new macrocyclic compounds, macrosphelides were discovered in the culture of a fungal strain Microsphaeropsis sp. FO-5050. Macrosphelides are the first 16-membered-ring microbial metabolite embodying three ester linkages and showed anti-cell-adherent activity. Therefore, macrosphelides became a target for total synthesis around the globe. Recently, new biological activity of macrosphelides has been reported, which brings a new dimension. In the paper, the discovery, biological activity and total synthesis of macrosphelides, and their recent history are described.
