Design, synthesis, and biophysical and biological evaluation of a series of pyrrolobenzodiazepine-poly(N-methylpyrrole) conjugates.

@article{Wells2006DesignSA,
  title={Design, synthesis, and biophysical and biological evaluation of a series of pyrrolobenzodiazepine-poly(N-methylpyrrole) conjugates.},
  author={Geoff Wells and Christopher R. H. Martin and Philip Howard and Zara A. Sands and Charles A. Laughton and Arnaud C Tiberghien and Chi Kit Woo and Luke Masterson and M Stephenson and John A. Hartley and Terence C. Jenkins and Steven D. Shnyder and Paul M. Loadman and Michael J. Waring and David E. Thurston},
  journal={Journal of medicinal chemistry},
  year={2006},
  volume={49 18},
  pages={
          5442-61
        }
}
A novel series of methyl ester-terminated C8-linked pyrrolobenzodiazepine (PBD)-poly(N-methylpyrrole) conjugates (50a-f) has been synthesized and their DNA interaction evaluated by thermal denaturation, DNA footprinting, and in vitro transcription stop assays. The synergistic effect of attaching a PBD unit to a polypyrrole fragment is illustrated by the large increase in DNA binding affinity (up to 50-fold) compared to the individual PBD and pyrrole components. 50a-f were found to bind mainly… 
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