title: Inhibition of malaria parasite growth by quinomycin A and its derivatives through DNA-intercalating activity.
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.
authors.affiliation: a Antibiotics Laboratory , RIKEN , Wako , Japan.
authors.forename: Hiroki
authors.initials: H
authors.lastname: Hayase
authors.forename: Nobumoto
authors.initials: N
authors.lastname: Watanabe
authors.forename: Chung Liang
authors.initials: CL
authors.lastname: Lim
authors.forename: Toshihiko
authors.initials: T
authors.lastname: Nogawa
authors.forename: Keisuke
authors.initials: K
authors.lastname: Komatsuya
authors.forename: Kiyoshi
authors.initials: K
authors.lastname: Kita
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Osada
mesh_terms: D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology*; D002738:Chloroquine / Q000494:pharmacology; D016054:DNA, Protozoan / Q000037:antagonists & inhibitors* / Q000737:chemistry; D055808:Drug Discovery; D004448:Echinomycin / Q000737:chemistry / Q000494:pharmacology*; D004912:Erythrocytes / Q000166:cytology / Q000187:drug effects / Q000469:parasitology; D006801:Humans; D020128:Inhibitory Concentration 50; D007364:Intercalating Agents / Q000737:chemistry / Q000494:pharmacology*; D007770:L-Lactate Dehydrogenase / Q000037:antagonists & inhibitors / Q000378:metabolism; D010957:Plasmids / Q000737:chemistry / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000201:enzymology / Q000254:growth & development; D015800:Protozoan Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D054852:Small Molecule Libraries / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000962:Antimalarials; D016054:DNA, Protozoan; D007364:Intercalating Agents; D015800:Protozoan Proteins; D054852:Small Molecule Libraries; D004448:Echinomycin; D002738:Chloroquine; D007770:L-Lactate Dehydrogenase
keywords: DNA intercalation; antimalarial agents; quinomycin A