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

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

  • J Med Chem. 2005 Aug 25;48(17):5412-4. doi: 10.1021/jm0504151.
Laëtitia Bouérat 1,  Jef Fensholdt,  Xifu Liang,  Sophie Havez,  Simon F Nielsen,  Jens R Hansen,  Simon Bolvig,  Christina Andersson
Affiliations

Affiliation

  • 1 LEO Pharma A/S, Industriparken, DK-2750 Ballerup, Denmark. laetitia.bouerat@leo-pharma.com
PMID: 16107139 DOI: 10.1021/jm0504151
Abstract

The known VEGFR2/KDR/Flk-1 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.

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