LAUSR

To find potent chemotherapeutic agents, cytotoxic effects of 42 synthetic chalcone derivatives bearing naphthyl groups on HCT116 human colon cancer cell lines were tested using the clonogenic long-term survival assay. The relationships between their half-maximal cell growth inhibitory concentrations (GI50) and structural properties were obtained using comparative molecular field analysis and comparative molecular similarity indices analysis. The structural conditions that showed maximum cytotoxic effects on the colon cancer cells were determined. In addition, a derivative, (E)-1-(2-hydroxy-4,5-dimethoxyphenyl)-3-(naphthalen-1-yl)prop-2-en-1-one, showing the best GI50 value, was assessed for stimulating reactive oxygen species (ROS) production. While its treatment on non-tumorigenic epithelial MCF-12A cell line did not affect the intracellular ROS levels, its treatment on MDA-MB-231 human breast cancer cell line showed ROS accumulation. These findings demonstrate that naphthalenylchalcones can be developed as potent chemotherapeutic agents.