Inhibition of DNA topoisomerases II and/or I by pyrazolo[1,5-a]indole derivatives and their growth inhibitory activities.

@article{Umemura2002InhibitionOD,
  title={Inhibition of DNA topoisomerases II and/or I by pyrazolo[1,5-a]indole derivatives and their growth inhibitory activities.},
  author={Ken Umemura and Tomoko Mizushima and Hajime Katayama and Yoshimitsu Kiryu and Takao Yamori and Toshiwo Andoh},
  journal={Molecular pharmacology},
  year={2002},
  volume={62 4},
  pages={873-80}
}
DNA topoisomerases (topos) I and II are molecular targets of several potent anticancer agents. Thus inhibitors of these enzymes are potential candidates or model compounds for anticancer drugs. We found some of the totally synthetic pyrazolo[1,5-a]indole derivatives, GS-2, -3, and -4, to be strong inhibitors of topo II, and GS-5 was found to be a dual inhibitor of topos I and II (IC(50) values were in the range of 10-30 microM). Because of the DNA-intercalating activity of these compounds… CONTINUE READING
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References

Publications referenced by this paper.
Showing 1-10 of 35 references

Antitumour activity of a novel quinolone derivative , TAS103 , with inhibitory effects on topoisomerases I and II

  • T Utsugi, K Aoyagi, +5 authors Y Yamada
  • Jpn J Cancer Res
  • 1997
Highly Influential
4 Excerpts

Antitumour activity of a novel quinolone derivative, TAS-103, with inhibitory effects on topoisomerases

  • T Utsugi, K Aoyagi, +5 authors Y Yamada
  • I and II. Jpn J Cancer Res
  • 1997
Highly Influential
6 Excerpts

DNA topoisomerases

  • JC Wang
  • Annu Rev Biochem 65:635–692
  • 1996
Highly Influential
4 Excerpts

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