Microtubules are a valid target for anticancer drugs, and it is important to continue developing those antimitotic drugs as chemotherapeutic agent. It has been reported that some natural flavonoids (2-phenyl-4-quinolone) exert potent cytoxicity activity against several cancer cell lines by inhibiting microtubule dynamics. The enhanced antimitotic compound of 2-phenyl-4-quinolone has strong antimitotic effects and specifically interacts with the colchicine biding site on β tubulin. 2-phenyl-4-quinolone derivative was reported as antitumor agents during the past 13 years. These effective compounds were evaluated against most human cancer cell lines both in vitro and in vivo. CWF-145, a synthetic 2-phenyl-4-quinolone derivative, was identified as a potent antitumor agent in human prostate cancer PC3 cell line. CWF-145 induced growth inhibition and apoptosis in a time- and concentration- dependent manner with an IC50 value about 100nM, but did not obviously impair the viability of normal cells for mouse fibroblast NIH3T3 cell line. We compared the toxicity of antimitotic compounds used in clinical practice such as taxol and doxorubicin with CWF-145, and CWF-145 had a low toxicity. CWF-145 caused cell cycle arrest at G2/M phase by interfering with tubulin polymerization and disrupted microtubule organization. Thus, CWF-145 could suppress PC3 cell growth via mitotic phase arrest and is worthy to further investigation as antitumor agent.
