The Scripps Research Institute

N Paul King

Kyriacos Costa Nicolaou

Yun He

Sacha Ninkovic

Dionisios Vourloumis

Frank Roschangar

Hans Vallberg

Francisco Sarabia

M Ray Finlay

Nicolas Winssinger

Zhen Yang

Tianhu Li

Joaquin Pastor

David Hepworth

Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancer agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of microtubulin assembly. The analogs of epothilone are novel. Several of the anlogs are demonstrated to have a superior cytotoxic activities as compared to epothilone A or epothilone B as demonstrated by their enhanced ability to induce the polymerization and stabilization of microtubules.

Epothilone analogs

Novel analogs of epothilone A, epothilone B, and epothilone C are synthesized by Stille coupling thazole-stannanes to macrolactone intermediates. The synthetic epothilone analogs selectively prevent mitosis in cancer cells through the induction and stabilization of microtubulin assembly. Selected synthetic epothilone analogs are demonstrated to have greater bioactivity than their corresponding native compound.

Growing community of inventors

San Diego, CA, United States of America

N Paul King