Chemistry & Biodiversity · 2005 · 149 citations · 5 references
PharmacyMedicinal ChemistryPharmacologyAntimicrobial PharmacologyDrug DiscoveryStructure-activity RelationshipsEnzyme InhibitionIn Vitro PharmacologyNatural Product Drug DiscoveryQualitative Structure-activity RelationshipsStructure-activity Relationship AnalysisAntimalarial AgentsAntimalarial ChemotherapyAntimalarial Drug DevelopmentChemotherapy Of MalariaPlasmodium FalciparumTreatment Of Malaria
The in vitro antiplasmodial activity of 26 naphthoquinone derivatives related to the natural lapachol (1) and beta-lapachone (2) was tested. Ten of these derivatives are reported for the first time. The evaluation was performed on cultures of F32 strain of Plasmodium falciparum, and some derivatives displayed attractive in vitro activities (IC50 < 10 microM). Based on these results, some structure-activity relationships have been determined.
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Human Malaria Parasites in Continuous Culture
William Trager, James B. Jensen · Science · 1976 · 8K citations