Rationally Designed Aromatase Inhibitors as Anti-Breast Cancer Agents

We have developed exemestane-based vinyl diazo compounds that act as aromatase inhibitors to be used in the treatment of cancer, particularly breast and ovarian cancer. Exemestane is structurally related to androstenedione and acts as an irreversible, steroidal aromatase inactivator. Our aromatase inhibitors are based upon the steroid scaffold and contain inserted alcohols and acids. Biological assessments of our compounds show improved inhibition, particularly those containing an alkyne derived side-chain.

Aromatase is over-expressed in >75% of breast cancer lines. The triazoles Letrozole and Anastrozole are used as current medications; however, current aromatase inhibitors are not specific with their target activity. This non-specific binding can increase the risk of bone disease. In addition, many patients that are chronically treated with tamoxifen and/or other aromatase inhibitors develop acquired resistance to these drugs. Our novel compounds would provide potential alternatives for treatment that are also specific with their target activity.

Developmental Stage & Potential Market

  • Additional testing is underway to investigate the stereoselectivity of the insertion site.
  • After prolonged treatments, acquired resistance to current aromatase inhibitors that are on the market is expected to occur in a majority of breast cancer patients.
  • Development of aromatase inhibitors with specific activity may decrease potentially debilitating side effects including bone loss.


  • Inhibits aromatase in a potent and specific manner.
  • Provides alternatives to the current medications that act as non-specific aromatase inhibitors
Patent Information:
Technology/Start-up ID: