Abstract:The basical structure of diketopiperazines is a cyclic dipeptide condensed by two amino acids. Because of the stable framework of the six-member ring structure, and having two hydrogen bond donor and two hydrogen bond receptor, DKPs have become important chemical pharmacophores, with strong biological activities and pharmacological activities in the drug. A series of cyclic compounds were found from marine organisms in recent years, research showed that their functions are not limited on anti-bacterial, cytotoxic activity, and so on, but also playing an important role in regulatory mechanism of quorum sensing as signal molecules, they have become research hot point in ecological chemistry. This paper reviewed the research progress of diketopiperazines found in the marine microbial metabolites, and the future study trends was discussed and outlooked.