Artemisinin-polypyrrole conjugates: synthesis, DNA binding studies and preliminary antiproliferative evaluation.

  • Louise LaPensée
  • , Sunil Sabbani
  • , Raman Sharma
  • , Inder Bhamra
  • , Emma Shore
  • , Amy E. Chadwick
  • , Neil G. Berry
  • , James Firman
  • , Nuna C. Araujo
  • , Lília Cabral
  • , Maria L.S. Cristiano
  • , Cerys Bateman
  • , Omar Janneh
  • , Adelina Gavrila
  • , Yi Hang Wu
  • , Afthab Hussain
  • , Steve Ward
  • , Paul A. Stocks
  • , Rick Cosstick
  • , Paul M. O'Neill

Research output: Contribution to journalArticlepeer-review

7 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)709-718
Number of pages10
JournalChemMedChem
Volume8
Issue number5
DOIs
Publication statusPublished - 1 May 2013

Keywords

  • Artemisinin
  • Binding studies
  • Cytotoxicity
  • DNA
  • Molecular modelling

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