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Short Paper | Regular issue | Vol 85, No. 5, 2012, pp.1179-1185
Published online, 22nd March, 2012
DOI: 10.3987/COM-12-12446
New Synthesis of Pyrvinium That inhibits the β-Catenin/Tcf4 Pathway

Yongjun Mao, Nan Lin, Wang Tian, Ziwei Huang, and Jing An*

*Department of Pharmacology, Upstate Medical University, State University of New York, 750 East Adams Street, Syracuse, NY 13210, U.S.A.


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 Friedländer 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 β-catenin/Tcf4 driven TOP-luciferase activity, with an IC50 value < 1 µM, and induces colon cancer cell death in a dose-dependent manner with an IC50 of 0.54 ± 0.06 µM.