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Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood-brain barrier permeability.
Borsari, Chiara; Keles, Erhan; Treyer, Andrea; De Pascale, Martina; Hebeisen, Paul; Hamburger, Matthias; Wymann, Matthias P.
Afiliación
  • Borsari C; Department of Biomedicine, University of Basel Mattenstrasse 28 4058 Basel Switzerland Matthias.Wymann@Unibas.ch.
  • Keles E; Department of Biomedicine, University of Basel Mattenstrasse 28 4058 Basel Switzerland Matthias.Wymann@Unibas.ch.
  • Treyer A; Pharmaceutical Biology, Pharmacenter, University of Basel Klingelbergstrasse 50 4056 Basel Switzerland.
  • De Pascale M; Department of Biomedicine, University of Basel Mattenstrasse 28 4058 Basel Switzerland Matthias.Wymann@Unibas.ch.
  • Hebeisen P; Department of Biomedicine, University of Basel Mattenstrasse 28 4058 Basel Switzerland Matthias.Wymann@Unibas.ch.
  • Hamburger M; PIQUR Therapeutics AG Hochbergerstrasse 60 4057 Basel Switzerland.
  • Wymann MP; Pharmaceutical Biology, Pharmacenter, University of Basel Klingelbergstrasse 50 4056 Basel Switzerland.
RSC Med Chem ; 12(4): 579-583, 2021 Jan 12.
Article en En | MEDLINE | ID: mdl-34041490
Highly selective mTOR inhibitors have been discovered through the exploration of the heteroaromatic ring engaging the binding affinity region in mTOR kinase. Compound 11 showed predicted BBB permeability in a MDCK-MDR1 permeability in vitro assay, being the first pyrimido-pyrrolo-oxazine with potential application in the treatment of neurological disorders.

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Tipo de estudio: Prognostic_studies / Risk_factors_studies Idioma: En Revista: RSC Med Chem Año: 2021 Tipo del documento: Article

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Tipo de estudio: Prognostic_studies / Risk_factors_studies Idioma: En Revista: RSC Med Chem Año: 2021 Tipo del documento: Article
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