These authors contributed equally to this work.
Artemisinin–Polypyrrole Conjugates: Synthesis, DNA Binding Studies and Preliminary Antiproliferative Evaluation
Article first published online: 11 MAR 2013
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Volume 8, Issue 5, pages 709–718, May 2013
How to Cite
La Pensée, L., Sabbani, S., Sharma, R., Bhamra, I., Shore, E., Chadwick, A. E., Berry, N. G., Firman, J., Araujo, N. C., Cabral, L., Cristiano, M. L. S., Bateman, C., Janneh, O., Gavrila, A., Wu, Y. H., Hussain, A., Ward, S. A., Stocks, P. A., Cosstick, R. and O'Neill, P. M. (2013), Artemisinin–Polypyrrole Conjugates: Synthesis, DNA Binding Studies and Preliminary Antiproliferative Evaluation. ChemMedChem, 8: 709–718. doi: 10.1002/cmdc.201200536
- Issue published online: 26 APR 2013
- Article first published online: 11 MAR 2013
- Manuscript Received: 19 NOV 2012
- British Engineering and Physical Sciences Research Council (EPSRC)
- EU FP6 Malaria Initiative ANTIMAL
- binding studies;
- molecular modelling
Greater than the sum of its parts: Artemisinins are currently in phase I–II clinical trials against breast, colorectal and non-small-cell lung cancers. In an attempt to offer increased specificity, a series of hybrid artemisinin–polypyrrole minor groove binder conjugates are described. DNA binding/modelling studies and preliminary biological evaluation give insights into their mechanism of action and the potential of this strategy.