Structure‐Activity Relationships of Chalcone Derivatives as Inhibitors of Breast Cancer Cell Growth

Abstract

Chalcones are polyphenols composed of two aromatic rings linked by an aliphatic three carbon chain. Chalcones and their derivatives have been shown to have numerous types of biological activity including anti‐inflammatory, antioxidant, anti‐infective, antiviral, anticancer and antitumor. Previous work in our lab discovered that anti‐cancer activity benefitted from electron donating substitutions to the B ring. Here, we are exploring the flexibility of the bridge structure using tetralone and indanone to generate a more rigid link between the aromatic rings. Using tetralone and indanone combined with benzaldehydes bearing carious electron donating groups a diverse library of chalcones was generated. These different compounds were first tested in noncancerous HEK 293 cells and have continued being tested in breast cancer cells (MCF7). An initial screening assay is performed at 50 μM. Compounds showing fifty percent or greater inhibition are taken on for more detailed analysis to determine an IC50. In both cases, cells are counted and seeded at specific densities, followed by drug treatment forty‐eight hours later, then cell viability is measured using an MTS assay on a visible spectrophotometer forty‐eight hours after drug treatment. Our results indicate the flexibility is an important feature for biological activity.Support or Funding InformationBellarmine University Chemistry and Physics DepartmentThis abstract is from the Experimental Biology 2019 Meeting. There is no full text article associated with this abstract published in The FASEB Journal.