|Title: ||Antiplasmodial activity of synthetic ellipticine derivatives and an isolated analog|
|Authors: ||Montoia, Andréia|
Silva, Luiz Francisco Rocha e
Torres, Zelina Estevam dos Santos
Costa, David Siqueira
Henrique, Marycleuma Campos
Lima, Emerson Silva
Vasconcellos, Marne Carvalho de
Souza, Rita C.Z.
Costa, Mônica Regina Farias
Grafov, Andrèi Andriy
Grafova, Iryna A.
Eberlin, M. N.
Tadei, Wanderli Pedro
Amorim, Rodrigo C.N.
Pohlit, Adrian Martin
|Keywords: ||2 Methyl 1,2,3,4 Tetrahydroellipticine|
2 Methyl 1,2,3,4 Tetrahydroellipticine
In Vitro Study
Carbon Nuclear Magnetic Resonance
Proton Nuclear Magnetic Resonance
Disease Models, Animals
|Issue Date: ||2014|
|metadata.dc.publisher.journal: ||Bioorganic and Medicinal Chemistry Letters|
|metadata.dc.relation.ispartof: ||Volume 24, Número 12, Pags. 2631-2634|
|Abstract: ||Ellipticine 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.|
|Appears in Collections:||Artigos|
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