Aromatase Inhibitors as Anti-Cancer Agents


Steroid-based vinyl diazo compounds for use in the treatment of cancer.

Key Benefits

  • Inhibits aromatase in a potent and specific manner.
  • Provides alternatives to the current medications that act as non-specific aromatase inhibitors.

Technical Summary

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

Additional testing is underway to investigate the stereoselectivity of the insertion site.

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Patent Information

App Type Country Serial No. Patent No. File Date Issued Date Patent Status
Nationalized PCT - Foreign EP 11766695.8   4/7/2011   Pending
Nationalized PCT - United States United States 13/635,924 8,969,327 9/19/2012 3/3/2015 Issued
Nationalized PCT - Foreign Australia 2011237592 2011237592 9/25/2012 2/9/2017 Issued
Nationalized PCT - Foreign Canada 2,794,565 2,794,565 9/25/2012 8/21/2018 Issued
Tech ID: 10097
Published: 11/24/2010

Jessica Beach
Marketing Specialist
Emory, OTT
(404) 727-1899

Huw Davies
Daniel Morton
Debashis Ghosh

Small Molecule