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†

Andrea Kurzwernhart,^ab Wolfgang Kandioller,^a Caroline Bartel,^a Simone Bächler,^c Robert Trondl,^a Gerhard Mühlgassner,^a Michael A. Jakupec,^ab Vladimir B. Arion,^ab Doris Marko,^c Bernhard K. Keppler^ab and Christian G. Hartinger*^abd

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* Corresponding authors

^a University of Vienna, Institute of Inorganic Chemistry, Währinger Str. 42, 1090 Vienna, Austria
E-mail: christian.hartinger@univie.ac.at
Fax: 43 1 4277 9526
Tel: 43 1 4277 52609

^b University of Vienna, Research Platform “Translational Cancer Therapy Research”, Währinger Str. 42, A-1090 Vienna, Austria

^c University of Vienna, Institute of Food Chemistry and Toxicology, Währinger Str. 38, 1090 Vienna, Austria

^d The University of Auckland, School of Chemical Sciences, Private Bag 92019, Auckland 1142, New Zealand

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.

Chemical Communications

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

Abstract

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

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