Targeting the DNA-topoisomerase complex in a double-strike approach with a topoisomerase inhibiting moiety and covalent DNA binder

Andrea Kurzwernhart; Wolfgang Kandioller; Caroline Bartel; Simone Bächler; Robert Trondl; Gerhard Mühlgassner; Michael A Jakupec; Vladimir B Arion; Doris Marko; Bernhard K Keppler; Christian G Hartinger

doi:10.1039/c2cc31040f

Targeting the DNA-topoisomerase complex in a double-strike approach with a topoisomerase inhibiting moiety and covalent DNA binder

Chem Commun (Camb). 2012 May 18;48(40):4839-41. doi: 10.1039/c2cc31040f. Epub 2012 Apr 12.

Authors

Andrea Kurzwernhart¹, Wolfgang Kandioller, Caroline Bartel, Simone Bächler, Robert Trondl, Gerhard Mühlgassner, Michael A Jakupec, Vladimir B Arion, Doris Marko, Bernhard K Keppler, Christian G Hartinger

Affiliation

¹ University of Vienna, Institute of Inorganic Chemistry, Währinger Str. 42, 1090 Vienna, Austria.

PMID: 22498692
DOI: 10.1039/c2cc31040f

Abstract

Ru(II)(arene)-flavonoids with high in vitro antitumour activity were synthesised. These compounds are capable of inhibiting human topoisomerase IIα and binding covalently to DNA.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antigens, Neoplasm / metabolism*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology
Cell Line, Tumor
Cell Survival / drug effects
Coordination Complexes / chemistry
Coordination Complexes / pharmacology
DNA / metabolism*
DNA Topoisomerases, Type II / metabolism*
DNA-Binding Proteins / antagonists & inhibitors
DNA-Binding Proteins / metabolism*
Flavonoids / chemistry
Humans
Molecular Conformation
Protein Binding
Ruthenium / chemistry

Substances

Antigens, Neoplasm
Antineoplastic Agents
Coordination Complexes
DNA-Binding Proteins
Flavonoids
Ruthenium
DNA
DNA Topoisomerases, Type II