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Investigation of morpholine isosters for the development of a potent, selective and metabolically stable mTOR kinase inhibitor.
De Pascale M, Bissegger L, Tarantelli C, Beaufils F, Prescimone A, Mohamed Seid Hedad H, Kayali O, Orbegozo C, Raguž L, Schaefer T, Hebeisen P, Bertoni F, Wymann MP, Borsari C. De Pascale M, et al. Eur J Med Chem. 2023 Feb 15;248:115038. doi: 10.1016/j.ejmech.2022.115038. Epub 2022 Dec 28. Eur J Med Chem. 2023. PMID: 36634458 Free article.
Covalent Proximity Scanning of a Distal Cysteine to Target PI3Kα.
Borsari C, Keles E, McPhail JA, Schaefer A, Sriramaratnam R, Goch W, Schaefer T, De Pascale M, Bal W, Gstaiger M, Burke JE, Wymann MP. Borsari C, et al. Among authors: de pascale m. J Am Chem Soc. 2022 Apr 13;144(14):6326-6342. doi: 10.1021/jacs.1c13568. Epub 2022 Mar 30. J Am Chem Soc. 2022. PMID: 35353516 Free PMC article.
4-(Difluoromethyl)-5-(4-((3R,5S)-3,5-dimethylmorpholino)-6-((R)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders.
Borsari C, Keles E, Rageot D, Treyer A, Bohnacker T, Bissegger L, De Pascale M, Melone A, Sriramaratnam R, Beaufils F, Hamburger M, Hebeisen P, Löscher W, Fabbro D, Hillmann P, Wymann MP. Borsari C, et al. Among authors: de pascale m. J Med Chem. 2020 Nov 25;63(22):13595-13617. doi: 10.1021/acs.jmedchem.0c00620. Epub 2020 Nov 9. J Med Chem. 2020. PMID: 33166139 Free article.
50 results