Enediyne antibiotics and their models: new potential of acetylene chemistry

Structures and chemical properties of enediynes, viz., compounds comprising a system of conjugated double and triple bonds, are surveyed. The presence of this system in the molecules of enediyne antitumour antibiotics ensures their high activity. The mechanism of biological action of enediynes is discussed based on cycloaromatisation of the enediyne chromophore resulting in highly active benzenoid 1,4-diradicals, which selectively cleave DNA. The key strategies of enediyne synthesis are analysed.