We thank A. Perner for MS analysis, H. Heinecke for NMR measurements, T. Palenta for assistance in synthesis and E.-M. Neumann for assistance in biological assays. This work was supported by the Federal Ministry of Science and Technology (BMBF (Germany)).
Rational Design of an Apoptosis-Inducing Photoreactive DNA Intercalator†
Article first published online: 6 MAY 2013
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Angewandte Chemie International Edition
Volume 52, Issue 24, pages 6185–6189, June 10, 2013
How to Cite
Ueberschaar, N., Dahse, H.-M., Bretschneider, T. and Hertweck, C. (2013), Rational Design of an Apoptosis-Inducing Photoreactive DNA Intercalator. Angew. Chem. Int. Ed., 52: 6185–6189. doi: 10.1002/anie.201302439
- Issue published online: 5 JUN 2013
- Article first published online: 6 MAY 2013
- Manuscript Received: 23 MAR 2013
- Federal Ministry of Science and Technology (BMBF (Germany))
- antitumor agents;
- streptomyces chartreusis
Light on DNA intercalators: Molecular modeling and mutasynthesis were employed to rationally tailor the antitumoral agent chartreusin into a vinyl-substituted derivative. Exposure with visible light dramatically improved antiproliferative activities owing to covalent binding with DNA and induction of apoptosis. The results hold promise for a more efficient chemotherapy, in particular for selectively treating tumors with light probes.