Bioreductive activation of a series of indolequinones by human DT-diaphorase: structure-activity relationships.

@article{Phillips1999BioreductiveAO,
  title={Bioreductive activation of a series of indolequinones by human DT-diaphorase: structure-activity relationships.},
  author={Roger M. Phillips and Matthew A. Naylor and Mohammed Jaffar and Stephen W. Doughty and Steven A. Everett and Alison Breen and Guzanfar A Choudry and Ian James Stratford},
  journal={Journal of medicinal chemistry},
  year={1999},
  volume={42 20},
  pages={4071-80}
}
A series of indolequinones including derivatives of EO9 bearing various functional groups and related indole-2-carboxamides have been studied with a view to identifying molecular features which confer substrate specificity for purified human NAD(P)H:quinone oxidoreductase (DT-diaphorase), bioreductive activation to DNA-damaging species, and selectivity for DT-diaphorase-rich cells in vitro. A broad spectrum of substrate specificity exists, but minor changes to the indolequinone nucleus have a… CONTINUE READING