4.4 Article

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

Journal

RSC MEDICINAL CHEMISTRY
Volume 12, Issue 4, Pages 579-583

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/d0md00408a

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Highly selective mTOR inhibitors have been discovered by exploring the interaction of the heteroaromatic ring with the binding affinity region of mTOR kinase. Compound 11, the first pyrimido-pyrrolo-oxazine with potential application in the treatment of neurological disorders, demonstrated predicted BBB permeability in an in vitro MDCK-MDR1 permeability assay.
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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