Abstract: | Only a few months after the disclosure of the absolute configuration of epothilones A (R=H, see picture on the right) and B (R=Me) the first total syntheses of these natural products were reported. Interest intensified with the realization of their potential as anticancer agents with a taxol-like mechanism of action. In addition to describing the most important total syntheses and biological properties of the naturally occurring epothilones A–E, this review also provides a systematic overview of numerous epothilone analogues that have been modified in the A – D regions in order to obtain information about structure–activity relationships. |