Abstract
The use of amino acids as acyl substitutents at the 2-amino group of our benzophenone core structure yielded compounds with mainly good to moderate farnesyltransferase inhibitory and moderate antimalarial activity. However, these farnesyltransferase inhibitors display some degree of selectivity towards malarial parasites since there was no cytotoxic activity observed at 70-80 microM.
MeSH terms
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Amino Acids / chemistry
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Animals
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Antimalarials / chemical synthesis*
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Antimalarials / pharmacology*
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Benzophenones / chemical synthesis*
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Benzophenones / pharmacology*
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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Erythrocytes / parasitology
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Escherichia coli / drug effects
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Escherichia coli / enzymology
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HeLa Cells
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Humans
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Magnetic Resonance Spectroscopy
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Plasmodium falciparum / drug effects
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Plasmodium falciparum / growth & development
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Structure-Activity Relationship
Substances
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Amino Acids
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Antimalarials
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Benzophenones
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Enzyme Inhibitors