Phenolic lipids constitute a class of bioactive compounds comprising molecules having hydrophobic tails linked to a phenolic polar head, widely distributed in nature, with great variety of biological and industrial potential. The cytosporones, which are octaketide phenolic lipids, have been attracting the attention of many researchers owing to their biological potential, such as fungicidal, allelopathic, bactericidal and, cytotoxic activities. In 2008, it was noticed that the so-called cytosporone B specifically binds to the ligand-binding domain of Nur77 or TR3, and is a potent killer in agonist stimuli. Some research groups are constantly striving to synthesize cytosporones and, many works have been published since 2003. Recently, some new similar octaketides were isolated and a few synthetic approaches are reported in the literature. Many results point out that cytosporones are potential molecules to develop promising pharmaceutical and agrochemical agents.