NU 2017-120

INVENTORS
Regan Thomson*
Emily Robinson

SHORT DESCRIPTION
Development of a new class of small molecules for the treatment of cancer

ABSTRACT
According to the National Cancer Institute, cancer is among the leading causes of death worldwide. In 2012, there were 14 million new cases and 8.2 million cancer-related deaths worldwide. It is predicted that the number of new cancer cases will rise to 22 million within the next two decades. Despite medical advances, there remains a pressing need for the development of new treatments for all forms of cancer. Northwestern researchers have developed a novel class of polycyclic molecules that display high levels of cytotoxicity against many of the most lethal cancers. In the course of studies on the development of new strategies to access polycyclic molecules, they synthesized a suite of complex polycyclic structures. These compounds and several derivatives thereof were found to display potent activity in cell viability assays against a panel of cancer cell lines, including clinically relevant metastatic breast cancer. The tricyclic and bicyclic compounds are reminiscent in structure to naturally occurring terpene molecules, but are fully synthetic and are shown to kill a host of cancer cells in cell viability studies. IC50 values were determined for two specific compounds against MDA231 (breast cancer cells), ER041 and ER124, and were determined to be 40 nM and 1845 nM, respectively.

APPLICATIONS

• Cancer therapeutic
• Probe molecules to understand cancer biology

ADVANTAGES

• Easily prepared compounds
• Novel chemical space

IP STATUS
Issued US Patent No. 11,286,226

PUBLICATION
Robinson E and Thomson R (2018) A Strategy for the Convergent and Stereoselective Assembly of Polycyclic Molecules. Journal of American Chemical Society. 140: 1956-1965.