Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596251 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
Topoisomerase II is a validated target in oncology. Among the different ways of blocking the function of this enzyme, inhibiting its ATPase activity has been relatively less investigated. In an effort to identify topoisomerase II inhibitors of a novel type, exerting their action by this mechanism, we have designed a purine inhibitor scaffold targeting the ATP-binding site of the enzyme. Searching the Novartis compound collection for molecules containing this purine motif has allowed the identification of two micromolar hits providing access to a new class of catalytic topoisomerase II inhibitors.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Pascal Furet, Joseph Schoepfer, Thomas Radimerski, Patrick Chène,