Targeting the DNA-topoisomerase complex in a double-strike approach with a topoisomerase inhibiting moiety and covalent DNA binder
A Kurzwernhart, W Kandioller, C Bartel… - Chemical …, 2012 - pubs.rsc.org
A Kurzwernhart, W Kandioller, C Bartel, S Bächler, R Trondl, G Mühlgassner, MA Jakupec…
Chemical Communications, 2012•pubs.rsc.org… In order to demonstrate the multi-targeted character of Ru II (flavone) complexes, we
studied the inhibition of human topoisomerase IIα activity and the binding ability to DNA
models. … In conclusion, the Ru II (arene)-flavonoid system offers access to multi-targeted
anticancer drugs consisting of a DNA binding metal centre and a biologically active ligand
system inhibiting topoisomerase IIα. With the accumulation in the endoplasmic reticulum as
a reservoir for the anticancer active moiety and the covalent binding to DNA accompanied …
studied the inhibition of human topoisomerase IIα activity and the binding ability to DNA
models. … In conclusion, the Ru II (arene)-flavonoid system offers access to multi-targeted
anticancer drugs consisting of a DNA binding metal centre and a biologically active ligand
system inhibiting topoisomerase IIα. With the accumulation in the endoplasmic reticulum as
a reservoir for the anticancer active moiety and the covalent binding to DNA accompanied …
RuII(arene)–flavonoids with high in vitro antitumour activity were synthesised. These compounds are capable of inhibiting human topoisomerase IIα and binding covalently to DNA.
The Royal Society of Chemistry