Use este identificador para citar ou linkar para este item: http://repositorio.inpa.gov.br/handle/123/4666
Título: Antiplasmodial activity of synthetic ellipticine derivatives and an isolated analog
Autor(es): MONTOIA, ANDREIA
GRAFOV, ANDRIY
GRAFOVA, IRYNA
EBERLIN, MARCOS N.
TADEI, WANDERLI P.
AMORIM, RODRIGO C.N.
Adrian Martin Pohlit
ROCHA E SILVA, LUIZ F.
TORRES, ZELINA E.
COSTA, DAVID S.
HENRIQUE, MARYCLEUMA C.
LIMA, EMERSON S.
VASCONCELLOS, MARNE C.
SOUZA, RITA C.Z.
COSTA, MONICA R.F.
Assunto: 2-metil-1,2,3,4-tetraidroelipticina
9-nitroelipticina
7-nitroelipticina
ISSN: 0960-894X
Revista: Bioorganic & Medicinal Chemistry Letters
Volume: 24
Resumo: 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.
URI: http://repositorio.inpa.gov.br/handle/123/4666
ISSN: 0960-894X
DOI: https://dx.doi.org/10.1016/j.bmcl.2014.04.070
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