Synthetic Inhibitors of DNA Topoisomerase I and II

Hajime KATAYAMA; Yusuke KAWADA; Kimiyoshi KANEKO; Takamitsu OSHIYAMA; Noriyuki TAKATSU

doi:10.1248/cpb.47.48

Hajime KATAYAMA, Yusuke KAWADA, Kimiyoshi KANEKO, Takamitsu OSHIYAMA, Noriyuki TAKATSU

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Keywords: dual inhibitor, DNA topoisomerase I, DNA topoisomerase II, pyrazolo[1, 5-a]indole, cytotoxicity, antitumor activity

JOURNAL FREE ACCESS

1999 Volume 47 Issue 1 Pages 48-53

DOI https://doi.org/10.1248/cpb.47.48

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Abstract

A new type of synthetic inhibitor of DNA topoisomerase I and II was examined and several of these derivatives exhibited strong dual activity against these enzymes. This series of compounds showed high cytotoxic activities against cancer cells, but only a limited number of compounds showed any noticeable activity in an in vivo test against murine P388. Non-specific toxicity was observed in the in vivo tests.

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