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

Literature Information

Publication Date 2021-01-12
DOI 10.1039/D0MD00408A
Impact Factor 0
Authors

Chiara Borsari, Erhan Keles, Andrea Treyer, Martina De Pascale, Matthias Hamburger, Matthias P. Wymann


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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. 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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