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.
Keywords: Antitumor agents; Epothilones; Natural products; Structure-activity relationships; Total synthesis.
© 1998 WILEY-VCH Verlag GmbH, Weinheim, Fed. Rep. of Germany.