Convenient Synthesis of Toxoflavin that Targets β‐Catenin/Tcf4 Signaling Activities |
| |
| Authors: | Yongjun Mao Wang Tian Ziwei Huang Jing An |
| |
| Institution: | 1. Department of Pharmacology, State University of New York, Upstate Medical University, Syracuse, New York;2. Upstate Cancer Research Institute, State University of New York, Upstate Medical University, Syracuse, New York |
| |
| Abstract: | A rapid and improved route for synthesis of toxoflavin, an antibiotic and antitumor agent, is described. The method uses easily obtained materials and simple and practical reactions, including chlorination, condensation, and diazotization to produce toxoflavin in five steps with 14.2% yield and 98.6% purity (HPLC). This synthetic toxoflavin effectively inhibited β‐catenin/Tcf4 driven TOP‐luciferase activity with an IC50 of less than 0.5 μM and induced colon cancer cell death in a dose‐dependent manner with an IC50 of 0.29 μM. |
| |
| Keywords: | |
|
|
