Abstract
Quinomycin A and its derivatives were identified as potent antimalarial (Plasmodium falciparum) agents in a screen of the RIKEN NPDepo chemical library. IC50 values of quinomycin A and UK-63,598 were approximately 100 times lower than that of the antimalarial drug chloroquine. This activity was mitigated by the addition of plasmid DNA, suggesting that these compounds act against parasites by intercalating into their DNA.
Keywords:
DNA intercalation; antimalarial agents; quinomycin A.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antimalarials / chemistry
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Antimalarials / pharmacology*
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Chloroquine / pharmacology
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DNA, Protozoan / antagonists & inhibitors*
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DNA, Protozoan / chemistry
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Drug Discovery
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Echinomycin / chemistry
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Echinomycin / pharmacology*
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Erythrocytes / cytology
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Erythrocytes / drug effects
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Erythrocytes / parasitology
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Humans
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Inhibitory Concentration 50
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Intercalating Agents / chemistry
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Intercalating Agents / pharmacology*
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L-Lactate Dehydrogenase / antagonists & inhibitors
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L-Lactate Dehydrogenase / metabolism
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Plasmids / chemistry
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Plasmids / pharmacology
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Plasmodium falciparum / drug effects*
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Plasmodium falciparum / enzymology
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Plasmodium falciparum / growth & development
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Protozoan Proteins / antagonists & inhibitors
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Protozoan Proteins / metabolism
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Small Molecule Libraries / chemistry
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Small Molecule Libraries / pharmacology
Substances
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Antimalarials
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DNA, Protozoan
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Intercalating Agents
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Protozoan Proteins
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Small Molecule Libraries
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Echinomycin
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Chloroquine
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L-Lactate Dehydrogenase