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Derivatives of 5-nitro-1H-benzo[de]isoquinoline-1,3(2H)-dione: design, synthesis, and biological activity

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Abstract

A series of mono and bis-2-(2-(dimethylamino)-ethyl)-5-nitro-1H-benzo[de]isoquinoline-1,3(2H)-diones with different amino side chains, a novel family of antitumor agents, has been designed and synthesized. Their antitumor activity was evaluated against HeLa, A549, P388, HL-60, MCF-7, HCT-8, and A375 cancer cell lines in vitro. Preliminary results showed that most of the derivatives had antitumor activity comparable with that of mitonafide, with IC 50 values of 10−6–10−5 M. More importantly, the derivatives had distinct antitumor selectivity against different cancer cell lines. This work provided a novel class of mitonafide-based lead compounds with improved antitumor selectivity against cancer cell lines for further optimization.

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Acknowledgments

This work was supported by the National Natural Science Foundation of China (90713026) and by Yangtze University.

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Authors and Affiliations

  1. College of Chemistry and Environmental Engineering, Yangtze University, 434023, Jingzhou, People’s Republic of China

    Aibin Wu, Jide Liu, Shaoxiong Qin & Ping Mei

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  1. Aibin Wu
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  2. Jide Liu
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  3. Shaoxiong Qin
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  4. Ping Mei
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Correspondence to Aibin Wu or Ping Mei.

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Wu, A., Liu, J., Qin, S. et al. Derivatives of 5-nitro-1H-benzo[de]isoquinoline-1,3(2H)-dione: design, synthesis, and biological activity. Monatsh Chem 141, 95–99 (2010). https://doi.org/10.1007/s00706-009-0220-9

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  • DOI: https://doi.org/10.1007/s00706-009-0220-9

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