Type II topoisomerase inhibitors

The invention relates to a family of selected 4-amino-2-pyrido bicyclic pyrimidines that inhibit human type II topoisomerase enzyme and that are useful as anticancer agents.

Patent title 4-amino-2-pyrido-bicyclic pyrimidines and use thereof as medicaments
Thematic area Health
Ownership Università degli Studi di Padova, ISTITUTO ITALIANO DI TECNOLOGIA - sede di Genova, ALMA MATER STUDIORUM - UNIVERSITA' DI BOLOGNA
Inventors Anna Minarini
Protection Europe, USA
Licensing status Available for development agreements, option, license and other exploitation agreements
Keywords Human type II topoisomerase, Topo II, Pyrimidines, Anticancer, Drug
Filed on 23 December 2016

Human type II topoisomerase enzymes (topo II) are essential for DNA topology modification, and represent a validated drug target to treat cancer. Several classes of topo II drugs have been developed over the last few decades. Although the existence of several topo II inhibitors, drug resistance and severe side effects related to topo II-targeted drugs, demand the discovery of novel and safer topo II inhibitors, toward better anticancer therapeutics.

The here proposed pyrimidines are potent inhibitors towards topo II and, at the same time, these compounds show promising results in blocking the proliferation of cancer cells.

- Described 4-amino-2-Pyrido bicyclic pyrimidines both efficiently inhibit topo II enzyme activity and reduce cancer cells proliferation (prostate and lung).

- The new structure is important for the drug-resistance tendency against known drugs.

Page published on: 10 April 2018