NEW SYNTHESIS OF PYRVINIUM THAT INHIBITS THE beta-CATENIN/TCF4 PATHWAY

[摘要]：A new and converged route is described for synthesis of pyrvinium, an anthelmintic and antitumor agent. This method uses easily obtained materials and simple and practical reactions, including the key Friedlander condensation, to form the quinoline ring. The final product is generated through eight steps, with 23% yield and 96.6% purity (HPLC). This synthetic pyrvinium effectively inhibits beta-catenin/Tcf4 driven TOP-luciferase activity, with an IC50 value < 1 mu M, and induces colon cancer cell death in a dose-dependent manner with an IC50 of 0.54 +/- 0.06 mu M.

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