Novel Fluoroindenoisoquinoline Non-Camptothecin Topoisomerase I Inhibitors

@article{Marzi2018NovelFN,
  title={Novel Fluoroindenoisoquinoline Non-Camptothecin Topoisomerase I Inhibitors},
  author={L. Marzi and K. Agama and J. Murai and S. Difilippantonio and A. James and C. Peer and W. Figg and D. Beck and M. S. Elsayed and M. Cushman and Y. Pommier},
  journal={Molecular Cancer Therapeutics},
  year={2018},
  volume={17},
  pages={1694 - 1704}
}
Contrary to other anticancer targets, topoisomerase I (TOP1) is targeted by only one chemical class of FDA-approved drugs: topotecan and irinotecan, the derivatives of the plant alkaloid, camptothecin. The indenoisoquinolines LMP400, LMP744, and LMP776 are novel noncamptothecin TOP1 inhibitors in clinical trial, which overcome the limitations of camptothecins. To further improve metabolic stability, their methoxy groups have been replaced by fluorine, as in the fluoroindenoisoquinolines NSC… Expand
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