Jump to main content
Jump to site search

Issue 7, 2015
Previous Article Next Article

Uncovering new structural insights for antimalarial activity from cost-effective aculeatin-like derivatives

Author affiliations

Abstract

A series of new aculeatin-like analogues were synthesized in two steps by combining two sets of building blocks. Many compounds showed inhibitory activities in vitro against Plasmodium falciparum and have helped to gain more insight into structure–activity relationships around the spirocyclohexadienone pharmacophoric scaffold. Plasmodium falciparum thioredoxin reductase (PfTrxR) has been investigated as a putative cellular target. Moreover, a new aculeatin-like scaffold without Michael acceptor properties, efficient at 0.86 μM against P. falciparum 3D7, was identified and raises the prospect of developing a new antimalarial agent.

Graphical abstract: Uncovering new structural insights for antimalarial activity from cost-effective aculeatin-like derivatives

Back to tab navigation

Supplementary files

Publication details

The article was received on 23 Nov 2014, accepted on 08 Dec 2014 and first published on 08 Dec 2014


Article type: Paper
DOI: 10.1039/C4OB02459A
Author version available: Download Author version (PDF)
Citation: Org. Biomol. Chem., 2015,13, 2064-2077
  •   Request permissions

    Uncovering new structural insights for antimalarial activity from cost-effective aculeatin-like derivatives

    M. Winkler, M. Maynadier, S. Wein, M. Lespinasse, G. Boumis, A. E. Miele, H. Vial and Y. Wong, Org. Biomol. Chem., 2015, 13, 2064
    DOI: 10.1039/C4OB02459A

Search articles by author

Spotlight

Advertisements