Chemical Biology of Epothilones

Angew Chem Int Ed Engl. 1998 Aug 17;37(15):2014-2045. doi: 10.1002/(SICI)1521-3773(19980817)37:15<2014::AID-ANIE2014>3.0.CO;2-2.

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.

Keywords: Antitumor agents; Epothilones; Natural products; Structure-activity relationships; Total synthesis.

Publication types

  • Review