Discovery of Potent Cell Migration Inhibitors through Total Synthesis: Lessons from Structure−Activity Studies of (+)-Migrastatin

Abstract

Synthesis of highly active migrastatin-based tumor migration cell inhibitors has been accomplished. Our flexible and concise total synthesis of migrastatin has allowed us to explore otherwise inaccessible migrastatin-derived structural motifs. This effort has resulted in the discovery of analogues with tumor cell migration inhibitory activity 3 orders of magnitude higher than that of the natural product.