Design and Synthesis of Chlorinated and Fluorinated 7-Azaindenoisoquinolines as Potent Cytotoxic Anticancer Agents That Inhibit Topoisomerase I.

@article{Elsayed2017DesignAS,
  title={Design and Synthesis of Chlorinated and Fluorinated 7-Azaindenoisoquinolines as Potent Cytotoxic Anticancer Agents That Inhibit Topoisomerase I.},
  author={M. S. Elsayed and Yafan Su and P. Wang and Taresh Sethi and K. Agama and A. Ravji and C. Redon and E. Kiselev and K. Horzmann and J. Freeman and Y. Pommier and M. Cushman},
  journal={Journal of medicinal chemistry},
  year={2017},
  volume={60 13},
  pages={
          5364-5376
        }
}
The 7-azaindenoisoquinolines are cytotoxic topoisomerase I (Top1) inhibitors. Previously reported representatives bear a 3-nitro group. The present report documents the replacement of the potentially genotoxic 3-nitro group by 3-chloro and 3-fluoro substituents, resulting in compounds with high Top1 inhibitory activities and potent cytotoxicities in human cancer cell cultures and reduced lethality in an animal model. Some of the new Top1 inhibitors also possess moderate inhibitory activities… Expand
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