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


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.

SUBMITTER: Borsari C 

PROVIDER: S-EPMC8128076 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature

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

Borsari Chiara C   Keles Erhan E   Treyer Andrea A   De Pascale Martina M   Hebeisen Paul P   Hamburger Matthias M   Wymann Matthias P MP  

RSC medicinal chemistry 20210112 4


Highly selective mTOR inhibitors have been discovered through the exploration of the heteroaromatic ring engaging the binding affinity region in mTOR kinase. Compound <b>11</b> showed predicted BBB permeability in a MDCK-MDR1 permeability <i>in vitro</i> assay, being the first pyrimido-pyrrolo-oxazine with potential application in the treatment of neurological disorders. ...[more]

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