Novel Furoquinolinediones as Inhibitors of TDP2 and Their Potential Use to Treat Cancer

The invention relates to novel Furoquinolinediones derivatives and their ability to inhibit the enzyme tyrosyl-DNA phosphodiesterase 2 (TDP2), and therefore to serve as anti-cancer agents. Furthermore, these compounds can be used in combination with topoisomerase II (Top2) inhibitors, such as etoposide or doxorubicin, to more effectively kill cancer cells in a synergistic fashion.  Pharmaceutical compositions containing these novel Furoquinolinediones and methods of treatment comprising administering of such compositions are disclosed in the invention.  Researchers at the NCI seek licensing and/or co-development research collaborations.

Potential Commercial Applications: Competitive Advantages:

• Furoquinolinediones derivatives can potentially be utilized for cancer treatment either as stand alone or in combination with other drugs such as Top2 inhibitors


• Combination therapies based on the association of a TDP2 and a Top2 inhibitor because of their synergistic effect should allow the decrease of the effective dosage. Their therapeutic benefit should be observed at non-toxic concentrations for normal cells as it has already been demonstrated for PARP inhibitors in BRCA-deficient tumors.

Development Stage:
Basic (Target Identification)


Yves Pommier (NCI)  ➽ more inventions...

Christophe Marchand (NCI)  ➽ more inventions...

Linkun An ()  ➽ more inventions...

Intellectual Property:
US Application No. 62/100,968

Collaboration Opportunity:

Licensing and research collaboration

Licensing Contact:
John Hewes, Ph.D.
Phone: 240-276-5515

OTT Reference No: E-275-2014
Updated: Oct 23, 2017