Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2014 Jun 15;24(12):2631-4.
doi: 10.1016/j.bmcl.2014.04.070. Epub 2014 Apr 28.

Antiplasmodial activity of synthetic ellipticine derivatives and an isolated analog

Affiliations

Antiplasmodial activity of synthetic ellipticine derivatives and an isolated analog

Andreia Montoia et al. Bioorg Med Chem Lett. .

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=0.55μM) exhibits greater antiplasmodial activity than ellipticine. These results are further evidence of the antimalarial potential of ellipticine derivatives.

Keywords: 2-Methyl-1,2,3,4-tetrahydroellipticine; 7,9-Dibromoellipticine; 7-Nitroellipticine; 9-Nitroellipticine; Plasmodium falciparum.

PubMed Disclaimer

Publication types

LinkOut - more resources