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.
Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood-brain barrier permeability / C. Borsari, E. Keles, A. Treyer, M. De Pascale, P. Hebeisen, M. Hamburger, M.P. Wymann. - In: RSC MEDICINAL CHEMISTRY. - ISSN 2632-8682. - 12:4(2021 Apr), pp. 579-583. [10.1039/d0md00408a]
Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood-brain barrier permeability
C. BorsariPrimo
;
2021
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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