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

Date Issued
2021-01-01
Author(s)
Borsari, Chiara  
Keles, Erhan  
Treyer, Andrea  
De Pascale, Martina  
Hebeisen, Paul  
Hamburger, Matthias  
Wymann, Matthias P.  
DOI
10.1039/d0md00408a
Abstract
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.
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