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.
• 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.
Yves Pommier (NCI), Christophe Marchand (NCI), Linkun An
- U.S. Patent Filed: U.S. Patent Application Number 62/100,968, Filed 08 Jan 2015