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

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 potent...

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Autores principales: Borsari, Chiara, Keles, Erhan, Treyer, Andrea, De Pascale, Martina, Hebeisen, Paul, Hamburger, Matthias, Wymann, Matthias P.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: RSC 2021
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8128076/
https://www.ncbi.nlm.nih.gov/pubmed/34041490
http://dx.doi.org/10.1039/d0md00408a
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author Borsari, Chiara
Keles, Erhan
Treyer, Andrea
De Pascale, Martina
Hebeisen, Paul
Hamburger, Matthias
Wymann, Matthias P.
author_facet Borsari, Chiara
Keles, Erhan
Treyer, Andrea
De Pascale, Martina
Hebeisen, Paul
Hamburger, Matthias
Wymann, Matthias P.
author_sort Borsari, Chiara
collection PubMed
description 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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spelling pubmed-81280762021-05-25 Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood–brain barrier permeability Borsari, Chiara Keles, Erhan Treyer, Andrea De Pascale, Martina Hebeisen, Paul Hamburger, Matthias Wymann, Matthias P. RSC Med Chem Chemistry 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. RSC 2021-01-12 /pmc/articles/PMC8128076/ /pubmed/34041490 http://dx.doi.org/10.1039/d0md00408a Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by-nc/3.0/
spellingShingle Chemistry
Borsari, Chiara
Keles, Erhan
Treyer, Andrea
De Pascale, Martina
Hebeisen, Paul
Hamburger, Matthias
Wymann, Matthias P.
Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood–brain barrier permeability
title Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood–brain barrier permeability
title_full Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood–brain barrier permeability
title_fullStr Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood–brain barrier permeability
title_full_unstemmed Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood–brain barrier permeability
title_short Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood–brain barrier permeability
title_sort second-generation tricyclic pyrimido-pyrrolo-oxazine mtor inhibitor with predicted blood–brain barrier permeability
topic Chemistry
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8128076/
https://www.ncbi.nlm.nih.gov/pubmed/34041490
http://dx.doi.org/10.1039/d0md00408a
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