Diaza- and triazachrysenes: potent topoisomerase-targeting agents with exceptional antitumor activity against the human tumor xenograft, MDA-MB-435.

@article{Ruchelman2002DiazaAT,
  title={Diaza- and triazachrysenes: potent topoisomerase-targeting agents with exceptional antitumor activity against the human tumor xenograft, MDA-MB-435.},
  author={Alexander L. Ruchelman and Sudhir K Singh and Xiaohua Wu and Abhijit Ray and Jin-ming Yang and T Li and Angela A Liu and Leroy F. Liu and Edmond J Lavoie},
  journal={Bioorganic & medicinal chemistry letters},
  year={2002},
  volume={12 22},
  pages={3333-6}
}
Several 5,12-diazachrysen-6-ones and 5,6,11-triazachrysen-12-ones were synthesized with varied substituents at the 5- or 11-position, respectively. Each compound was evaluated for its potential to stabilize the cleavable complex formed with TOP1 and DNA. Two analogues with very potent TOP1-targeting activity, 3a and 4a, exhibited cytotoxic activity with IC(50) values at or below 2nM against RPMI8402. Compound 3a was active in vivo by either ip or po administration in the human tumor xenograft… CONTINUE READING

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