Synthesis and evaluation of novel pyrimido-acridone,-phenoxadine, and-carbazole as topoisomerase II inhibitors

…, K Tsukahara, T Nagasu, N Koyanagi, K Kitoh…

Index: Kamata, Junichi; Okada, Toshimi; Kotake, Yoshihiko; Niijima, Jun; Nakamura, Katsuji; Uenaka, Toshimitsu; Yamaguchi, Atsumi; Tsukahara, Kappei; Nagasu, Takeshi; Koyanagi, Nozomu; Kitoh, Kyosuke; Yoshimatsu, Kentaro; Yoshino, Hiroshi; Sugumi, Hiroyuki Chemical and Pharmaceutical Bulletin, 2004 , vol. 52, # 9 p. 1071 - 1081

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Citation Number: 18

Abstract

As part of a series of studies to discover new topoisomerase II inhibitors, novel pyrimidoacridones, pyrimidophenoxadines, and pyrimidocarbazoles were synthesized, and in vitro and in vivo antitumor activities and DNA-protein and/or DNA-topoisomerase II cross- linking activity as an indicator of topoisomerase II-DNA cleavable complex formation were evaluated. The pyrimidocarbazoles possessed high in vitro and in vivo potencies. ...