Cytotoxic and DNA binding properties of aminoalkyl derivatives of di- and triazaphenanthrenes Academic Article uri icon

abstract

  • A series of mono- and dicationic derivatives of various di- and triazaphenanthrenes were synthesized and evaluated against both wild-type and amsacrine-resistant P388 leukemia in vitro. Monocationic derivatives of the fully-aromatic benzo[c][1,8]naphthyridine chromophore showed moderate and equal cytotoxicity in both cell lines, suggestive of efficacy against both the alpha and beta isozymes of mammalian DNA topoisomerase II. Derivatives of both the benzo[c][1,8]naphthyridine and benzo[c][1,8]naphthyridine-3(4H)-one chromophores also showed significant in vivo activity against wild-type P388 leukemia.

authors

  • Argiropoulos, G
  • Bates, MRM
  • Cherubim, P
  • Deady, LW
  • Ganakas, AM
  • Baguley, BC
  • Denny, WA

publication date

  • January 1, 1992