| Autor: |
Winkler M; Département de Pharmacochimie Moléculaire, Univ. Grenoble-Alpes, CNRS UMR 5063, CNRS ICMG FR 2607, bâtiment André Rassat, 470 rue de la Chimie, F-38041 Grenoble Cedex 9, France. yung-sing.wong@ujf-grenoble.fr., Maynadier M, Wein S, Lespinasse MA, Boumis G, Miele AE, Vial H, Wong YS |
| Jazyk: |
angličtina |
| Zdroj: |
Organic & biomolecular chemistry [Org Biomol Chem] 2015 Feb 21; Vol. 13 (7), pp. 2064-77. |
| DOI: |
10.1039/c4ob02459a |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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