Artemisinin–Polypyrrole Conjugates: Synthesis, DNA Binding Studies and Preliminary Antiproliferative Evaluation (pages 709–718)
Dr. Louise La Pensée, Dr. Sunil Sabbani, Dr. Raman Sharma, Dr. Inder Bhamra, Emma Shore, Dr. Amy E. Chadwick, Dr. Neil G. Berry, James Firman, Dr. Nuna C. Araujo, Lília Cabral, Prof. Maria L. S. Cristiano, Cerys Bateman, Dr. Omar Janneh, Adelina Gavrila, Yi Hang Wu, Afthab Hussain, Prof. Stephen A. Ward, Dr. Paul A. Stocks, Prof. Rick Cosstick and Prof. Paul M. O'Neill
Version of Record online: 11 MAR 2013 | DOI: 10.1002/cmdc.201200536
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.