Structure-activity relationships of saframycins

J Antibiot (Tokyo). 1984 Aug;37(8):847-52. doi: 10.7164/antibiotics.37.847.


In vitro antitumor activities of 13 saframycins, including the potent antitumor component, saframycin A, were determined with the highly sensitive established cell line of L1210 mouse leukemia to investigate structure-activity relationships. Saframycins which lack the alpha-cyanoamine group or the alpha-carbinolamine group exhibited much lower cytotoxic activity than saframycin A. The modification of active saframycins either at the C-14 position on the basic skeleton or at the C-25 position on the side chain with bulky substituents resulted in a decrease in cytotoxic activity. These structure-activity relationships corroborated the proposed major mechanism of action for the antitumor activity of saframycin A and supported our proposed model for the saframycin A-DNA adduct.

MeSH terms

  • Animals
  • Antibiotics, Antineoplastic*
  • Cell Line
  • Isoquinolines / pharmacology*
  • Leukemia L1210 / drug therapy
  • Magnetic Resonance Spectroscopy
  • Mice
  • Models, Molecular
  • Structure-Activity Relationship


  • Antibiotics, Antineoplastic
  • Isoquinolines