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Bioorg Med Chem Lett. 2009 Aug 1;19(15):4014-7. doi: 10.1016/j.bmcl.2009.06.034. Epub 2009 Jun 13.

Discovery of a new class of catalytic topoisomerase II inhibitors targeting the ATP-binding site by structure based design. Part I.

Author information

1
Novartis Institutes for BioMedical Research, WKL-136.P.12, CH-4002 Basel, Switzerland. pascal.furet@novartis.com

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.

PMID:
19560355
DOI:
10.1016/j.bmcl.2009.06.034
[Indexed for MEDLINE]
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