Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood-brain barrier permeability

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Abstract

Highly selective mTOR inhibitors have been discovered through the exploration of the heteroaromatic ring engaging the binding affinity region in mTOR kinase. Compound11showed predicted BBB permeability in a MDCK-MDR1 permeabilityin vitroassay, being the first pyrimido-pyrrolo-oxazine with potential application in the treatment of neurological disorders.

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Borsari, C., Keles, E., Treyer, A., De Pascale, M., Hebeisen, P., Hamburger, M., & Wymann, M. P. (2021). Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood-brain barrier permeability. RSC Medicinal Chemistry, 12(4), 579–583. https://doi.org/10.1039/d0md00408a

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