From a cytotoxic agent to the discovery of a novel antimalarial agent |
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| Authors: | Ravi S.P. Singh Umashankar Das Jennifer M. Auschwitz Susan E. Leed Mark R. Hickman Jonathan R. Dimmock Jane Alcorn |
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| Affiliation: | 1. Drug Design and Discovery Research Group, College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, Saskatchewan, Canada S7N 5C9;2. Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, MD 20910, USA |
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| Abstract: | A novel cytotoxin 3,5-bis(4-chlorobenzylidene)-1-[4-{2-(4-morpholinyl)ethoxy}phenyl-carbonyl]-4-piperidone hydrochloride 2 demonstrated potent antimalarial properties with IC50 values of 0.60 and 1.97 μM against the drug sensitive D6 strain and the C235 drug-resistant strain of Plasmodium falciparum. This compound concentrates in red blood cells, lowers glutathione concentrations in erythrocytes and permeates across CACO-2 cells. These data reveal 2 to be a promising lead compound in the quest for novel antimalarial agents. |
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