Antimalarial benzo[c]phenanthridines

James M. Nyangulu, Samantha L. Hargreaves, Susan L. Sharples, Simon P. Mackay, Roger D. Waigh, Olivier Duval, Eddie K. Mberu, William M. Watkins

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Abstract

Analogues of the antimalarial alkaloid nitidine have been prepared with high potency against both chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. Simple modifications, using an established synthetic route, resulted in an analogue with IC50 below 5 ng/mL against a chloroquine-sensitive strain of P. falciparum. N-Ethylethoxidine had IC50 below 30 ng/mL against both chloroquine-sensitive and chloroquine-resistant strains of P. falciparum.

Original languageEnglish
Pages (from-to)2007-2010
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number8
DOIs
Publication statusPublished - 15 Apr 2005

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Keywords

  • antimalarial
  • hloroquine-sensitive strain
  • hloroquine-resistant strain

Cite this

Nyangulu, J. M., Hargreaves, S. L., Sharples, S. L., Mackay, S. P., Waigh, R. D., Duval, O., ... Watkins, W. M. (2005). Antimalarial benzo[c]phenanthridines. Bioorganic and Medicinal Chemistry Letters , 15(8), 2007-2010. https://doi.org/10.1016/j.bmcl.2005.02.074