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

Chiara Borsari; Erhan Keles; Andrea Treyer; Martina De Pascale; Paul Hebeisen; Matthias Hamburger; Matthias P. Wymann

doi:10.1039/D0MD00408A

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

Chiara Borsari,

‡^a Erhan Keles,

‡^a Andrea Treyer,

^b Martina De Pascale,

^a Paul Hebeisen,^ac Matthias Hamburger

^b and Matthias P. Wymann

*^a

Author affiliations

* Corresponding authors

^a Department of Biomedicine, University of Basel, Mattenstrasse 28, 4058 Basel, Switzerland
E-mail: Matthias.Wymann@Unibas.ch

^b Pharmaceutical Biology, Pharmacenter, University of Basel, Klingelbergstrasse 50, 4056 Basel, Switzerland

^c PIQUR Therapeutics AG, Hochbergerstrasse 60, 4057 Basel, Switzerland

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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DOI: https://doi.org/10.1039/D0MD00408A
Article type: Research Article
Submitted: 04 Dec 2020
Accepted: 22 Dec 2020
First published: 12 Jan 2021
This article is Open Access

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RSC Med. Chem., 2021,12, 579-583

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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 and M. P. Wymann, RSC Med. Chem., 2021, 12, 579 DOI: 10.1039/D0MD00408A

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RSC Medicinal Chemistry

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

Abstract

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

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