The discovery of chlorothricin (1) defined a new family
of microbial metabolites with potent antitumor antibiotic properties
collectively referred to as spirotetronate polyketides. These microbial
metabolites are structurally distinguished by the presence of a spirotetronate
motif embedded within a macrocyclic core. Glycosylation at the periphery
of this core contributes to the structural complexity and bioactivity
of this motif. The spirotetronate family displays impressive chemical
structures, potent bioactivities, and significant pharmacological
potential. This review groups the family members based on structural
and biosynthetic considerations and summarizes synthetic and biological
studies that aim to elucidate their mode of action and explore their
pharmacological potential.