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Investigational New Drugs

, Volume 1, Issue 3, pp 213–218 | Cite as

Correlation of the structure of amino-substituted anthraquinones to cytotoxicity in cultured Chinese hamster cells

  • Bruce F. Kimler
  • C. C. Cheng
  • Richard E. Barnes
  • Mary L. Barnes
Preclinical

Summary

A number of substituted anthraquinones (SAQs) are currently being tested as cancer chemotherapeutic agents because of their structural similarity to Adriamycin (ADR) and other DNA-intercalating antibiotics. In this study, the effect of SAQs on the induction of cytotoxicity of asynchronous Chinese hamster cells in culture was studied and compared to those produced by ADR and dihydroxyanthraquinone (DHAQ), a SAQ previously shown to be more effective than ADR. SAQs produced cytotoxicity that was dependent upon the concentration and duration of drug exposure. A correlation was noted between the activity of a compound (the concentration required to produce a certain level of cell kill) and the presence of a particular triangular arrangement of one nitrogen atom and two oxygen atoms. There was also a correlation between chemical structure and antitumor activity in the murine P388 leukemia model system. This correlation between chemical structure and biological activity may aid in the development of new SAQs with greater potential as cancer chemotherapeutic agents.

Key words

substituted anthraquinones cytotoxicity structure-activity 

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Copyright information

© Martinus Nijhoff Publishers 1983

Authors and Affiliations

  • Bruce F. Kimler
    • 1
  • C. C. Cheng
    • 2
  • Richard E. Barnes
    • 1
  • Mary L. Barnes
    • 1
  1. 1.Radiation Biology Laboratory, Department of Radiation TherapyUniversity of Kansas Medical CenterKansas CityUSA
  2. 2.Radiation Biology Laboratory, Department of Pharmacology, Toxicology and TherapeuticsUniversity of Kansas Medical CenterKansas CityUSA

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