A new synthetic 2'-hydroxy-2,4,6-trimethoxy-5',6'-naphthochalcone induces G2/M cell cycle arrest and apoptosis by disrupting the microtubular network of human colon cancer cells.

Methoxylated chalcones exert antitumor activities. In the present study, we characterized the cytotoxicity of methylated chalcone derivatives against human colon cancer cells. We synthesized a group of methoxychalcones and explored the molecular mechanisms underlying inhibition of tumor growth by these materials. A new synthetic methoxychalcone, 2'-hydroxy-2,4,6-trimethoxy-5',6'-naphthochalcone (named HMNC-74), most effectively inhibited the clonogenicity of SW620 colon cancer cells. Mechanistically, HMNC-74 triggered cell cycle arrest at G2/M phase, followed by an increase in apoptotic cell death. Our results indicate that the cytotoxicity of the novel compound HMNC-74 involves the disruption of microtubular networks.