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dc.contributor.authorMontoia, Andréia-
dc.contributor.authorSilva, Luiz Francisco Rocha e-
dc.contributor.authorTorres, Zelina Estevam dos Santos-
dc.contributor.authorCosta, David Siqueira-
dc.contributor.authorHenrique, Marycleuma Campos-
dc.contributor.authorLima, Emerson Silva-
dc.contributor.authorVasconcellos, Marne Carvalho de-
dc.contributor.authorSouza, Rita C.Z.-
dc.contributor.authorCosta, Mônica Regina Farias-
dc.contributor.authorGrafov, Andrèi Andriy-
dc.contributor.authorGrafova, Iryna A.-
dc.contributor.authorEberlin, M. N.-
dc.contributor.authorTadei, Wanderli Pedro-
dc.contributor.authorAmorim, Rodrigo C.N.-
dc.contributor.authorPohlit, Adrian Martin-
dc.date.accessioned2020-06-15T21:48:29Z-
dc.date.available2020-06-15T21:48:29Z-
dc.date.issued2014-
dc.identifier.urihttps://repositorio.inpa.gov.br/handle/1/17604-
dc.description.abstractEllipticine has been shown previously to exhibit excellent in vitro antiplasmodial activity and in vivo antimalarial properties that are comparable to those of the control drug chloroquine in a mouse malaria model. Ellipticine derivatives and analogs exhibit antimalarial potential however only a few have been studied to date. Herein, ellipticine and a structural analog were isolated from Aspidosperma vargasii bark. A-ring brominated and nitrated ellipticine derivatives exhibit good in vitro inhibition of Plasmodium falciparum K1 and 3D7 strains. Several of the compounds were found not to be toxic to human fetal lung fibroblasts. 9-Nitroellipticine (IC50 = 0.55 μM) exhibits greater antiplasmodial activity than ellipticine. These results are further evidence of the antimalarial potential of ellipticine derivatives. © 2014 Elsevier Ltd. All rights reserved.en
dc.language.isoenpt_BR
dc.relation.ispartofVolume 24, Número 12, Pags. 2631-2634pt_BR
dc.rightsRestrito*
dc.subject2 Methyl 1,2,3,4 Tetrahydroellipticineen
dc.subject3,4 Dihydroellipticineen
dc.subject7 Nitroellipticineen
dc.subject7,8,9 Tribromoellipticineen
dc.subject7,9 Dibromoellipticineen
dc.subject9 Bromoellipticineen
dc.subject9 Hydroxyellipticineen
dc.subject9 Methoxyellipticineen
dc.subject9 Nitroellipticineen
dc.subjectAntimalarial Agenten
dc.subjectChloroquineen
dc.subjectEllipticineen
dc.subjectEllipticine Derivativeen
dc.subjectOlivacineen
dc.subjectUnclassified Drugen
dc.subjectAntimalarial Agenten
dc.subjectChloroquineen
dc.subjectEllipticineen
dc.subjectEllipticine Derivativeen
dc.subject2 Methyl 1,2,3,4 Tetrahydroellipticineen
dc.subject7 Nitroellipticineen
dc.subject7,9 Dibromoellipticineen
dc.subject9 Nitroellipticineen
dc.subjectAntimalarial Agenten
dc.subjectChloroquineen
dc.subjectEllipticineen
dc.subjectEllipticine Derivativeen
dc.subjectOlivacineen
dc.subjectQuinine Sulfateen
dc.subjectAntimalarial Activityen
dc.subjectAspidospermaen
dc.subjectAspidosperma Vargasiien
dc.subjectBarken
dc.subjectBrominationen
dc.subjectControlled Studyen
dc.subjectDrug Cytotoxicityen
dc.subjectDrug Effecten
dc.subjectDrug Isolationen
dc.subjectDrug Potencyen
dc.subjectFetusen
dc.subjectHumanen
dc.subjectHuman Cellen
dc.subjectIc 50en
dc.subjectIn Vitro Studyen
dc.subjectLung Fibroblasten
dc.subjectMedicinal Planten
dc.subjectNitrationen
dc.subjectNonhumanen
dc.subjectPlasmodium Bergheien
dc.subjectPlasmodium Falciparumen
dc.subjectAnimalsen
dc.subjectChemical Structureen
dc.subjectChemistryen
dc.subjectDisease Modelen
dc.subjectDrug Effectsen
dc.subjectFibroblasten
dc.subjectMouseen
dc.subjectSynthesisen
dc.subjectAnimals Cellen
dc.subjectAnimals Experimenten
dc.subjectAnimals Modelen
dc.subjectAntiplasmodial Activityen
dc.subjectAspidospermaen
dc.subjectAspidosperma Vargasiien
dc.subjectCarbon Nuclear Magnetic Resonanceen
dc.subjectDrug Structureen
dc.subjectDrug Synthesisen
dc.subjectMacrophageen
dc.subjectMalariaen
dc.subjectMalaria Controlen
dc.subjectMass Spectrometryen
dc.subjectParasitemiaen
dc.subjectProton Nuclear Magnetic Resonanceen
dc.subjectAspidospermaen
dc.subjectPlasmodium Falciparumen
dc.subjectAnimalen
dc.subjectAntimalarialsen
dc.subjectAspidospermaen
dc.subjectChloroquineen
dc.subjectDisease Models, Animalsen
dc.subjectEllipticinesen
dc.subjectFibroblastsen
dc.subjectHumansen
dc.subjectMiceen
dc.subjectMolecular Structureen
dc.subjectPlant Barken
dc.subjectPlasmodium Falciparumen
dc.titleAntiplasmodial activity of synthetic ellipticine derivatives and an isolated analogen
dc.typeArtigopt_BR
dc.identifier.doi10.1016/j.bmcl.2014.04.070-
dc.publisher.journalBioorganic and Medicinal Chemistry Letterspt_BR
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