Hydroxy-anthraquinones as antimalarial agents

R. W. Winter, Kenneth A. Cornell, Linda L. Johnson, Loren M. Isabelle, David J. Hinrichs, Michael K. Riscoe

Research output: Contribution to journalArticle

20 Scopus citations

Abstract

A series of hydroxy- and polyhydroxy-anthraquinones were screened for inhibitory activity against the malarial parasite, Plasmodium falciparum. Rufigallol demonstrated the most potent effects with a 50% inhibitory concentration (IC50 value of ∼10.5 ng/ml (∼35 nM). Deleterious effects were exerted by rufigallol toward bone marrow progenitor cells at concentrations≥ 10 μM (3 μg/ml) where ∼30% suppression of colony growth was noted. Taking into consideration its potency and relative lack of toxicity, we believe that rufigallol should be advanced for in vivo studies. At the very least, rufigallol represents a simple, inexpensive lead drug for the development of more potent analogs.

Original languageEnglish (US)
Pages (from-to)1927-1932
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume5
Issue number17
DOIs
StatePublished - Sep 7 1995

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    Winter, R. W., Cornell, K. A., Johnson, L. L., Isabelle, L. M., Hinrichs, D. J., & Riscoe, M. K. (1995). Hydroxy-anthraquinones as antimalarial agents. Bioorganic and Medicinal Chemistry Letters, 5(17), 1927-1932. https://doi.org/10.1016/0960-894X(95)00326-O