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.
|Publication status||Published - 2013|
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This is the peer reviewed version of the following article: 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, volume 8 (5): 709-718, which has been published in final form at http://dx.doi.org/10.1002/cmdc.201200536. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for self-archiving.
- binding studies
- molecular modelling