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.

Title of the patent 4-amino-2-pyrido-bicyclic pyrimidines and use thereof as medicaments
Thematic area Pharmaceutical
Ownership Alma Mater Studiorum Università di Bologna, Fondazione Istituto Italiano di Tecnologia, Università degli Studi di Padova
Inventors Anna Minarini, Marco De Vivo, Jose Antonio Ortega Martinez, Jose Manuel Arenciba Jimenez, Claudia Sissi
Protection International
Licensing status Available for licensing agreement
Keywords Human type II topoisomerase, Topo II, pyrimidines, anticancer, drug
Filed on Dec 23, 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.