Indolin-2-ones with high in vivo efficacy in a model for multiple sclerosis.

Autor: Bouérat L; LEO Pharma A/S, Industriparken, DK-2750 Ballerup, Denmark. laetitia.bouerat@leo-pharma.com, Fensholdt J, Liang X, Havez S, Nielsen SF, Hansen JR, Bolvig S, Andersson C
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 2005 Aug 25; Vol. 48 (17), pp. 5412-4.
DOI: 10.1021/jm0504151
Abstrakt: The known KDR inhibitor SU5416 and several analogues of the indolin-2-one family were surprisingly found to be highly efficacious in the EAE model, an established model for multiple sclerosis. The high in vivo effect could be correlated to in vitro inhibition of the pro-inflammatory cytokine IL-2. Activity following po administration was obtained with several analogues and via the use of prodrugs.
Databáze: MEDLINE