New developments in antitumor anthracyclines

Pharmacol Ther. Oct-Dec 1997;76(1-3):117-24. doi: 10.1016/s0163-7258(97)00096-x.


Doxorubicin is a major anticancer agent introduced to extended clinical use in the early 1970s. The fulfillment of a wide program of analogue synthesis led to the development of the better tolerated epirubicin and of a highly potent antileukemic drug, idarubicin. In recent years, on the basis of the available information on the molecular requirements for action, a new synthetic program, coupled with target-oriented pharmacological experiments, was carried out. Various interesting derivatives, namely, the 8- and 10-fluoro compounds and the disaccharides, were obtained. The latter compounds exhibited a strong dependence of biological activity on the orientation (axial vs. equatorial) of the second sugar moiety, daunosamine. A member of this group, namely, 7-O-(4'-O-alpha-L-daunosaminyl-2'-deoxy-alpha-L-fucosyl)-4-demetho xy-adriamycinone, is presently undergoing clinical trials as a third generation antitumor anthracycline.

Publication types

  • Review

MeSH terms

  • Animals
  • Antibiotics, Antineoplastic / chemical synthesis*
  • Antibiotics, Antineoplastic / therapeutic use
  • Doxorubicin / analogs & derivatives*
  • Doxorubicin / chemistry*
  • Doxorubicin / therapeutic use
  • Drug Design
  • Humans
  • Models, Molecular
  • Structure-Activity Relationship


  • Antibiotics, Antineoplastic
  • Doxorubicin