146 related articles for article (PubMed ID: 36634458)
1. 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
Eur J Med Chem; 2023 Feb; 248():115038. PubMed ID: 36634458
[TBL] [Abstract][Full Text] [Related]
2. 4-(Difluoromethyl)-5-(4-((3
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
J Med Chem; 2020 Nov; 63(22):13595-13617. PubMed ID: 33166139
[TBL] [Abstract][Full Text] [Related]
3. Chemical and Structural Strategies to Selectively Target mTOR Kinase.
Borsari C; De Pascale M; Wymann MP
ChemMedChem; 2021 Sep; 16(18):2744-2759. PubMed ID: 34114360
[TBL] [Abstract][Full Text] [Related]
4. Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.
Rageot D; Bohnacker T; Melone A; Langlois JB; Borsari C; Hillmann P; Sele AM; Beaufils F; Zvelebil M; Hebeisen P; Löscher W; Burke J; Fabbro D; Wymann MP
J Med Chem; 2018 Nov; 61(22):10084-10105. PubMed ID: 30359003
[TBL] [Abstract][Full Text] [Related]
5. (
Rageot D; Bohnacker T; Keles E; McPhail JA; Hoffmann RM; Melone A; Borsari C; Sriramaratnam R; Sele AM; Beaufils F; Hebeisen P; Fabbro D; Hillmann P; Burke JE; Wymann MP
J Med Chem; 2019 Jul; 62(13):6241-6261. PubMed ID: 31244112
[TBL] [Abstract][Full Text] [Related]
6. A Kinase Inhibitor Targeted to mTORC1 Drives Regression in Glioblastoma.
Fan Q; Aksoy O; Wong RA; Ilkhanizadeh S; Novotny CJ; Gustafson WC; Truong AY; Cayanan G; Simonds EF; Haas-Kogan D; Phillips JJ; Nicolaides T; Okaniwa M; Shokat KM; Weiss WA
Cancer Cell; 2017 Mar; 31(3):424-435. PubMed ID: 28292440
[TBL] [Abstract][Full Text] [Related]
7. New inhibitors of the PI3K-Akt-mTOR pathway: insights into mTOR signaling from a new generation of Tor Kinase Domain Inhibitors (TORKinibs).
Feldman ME; Shokat KM
Curr Top Microbiol Immunol; 2010; 347():241-62. PubMed ID: 20549474
[TBL] [Abstract][Full Text] [Related]
8. Brain-penetrant PQR620 mTOR and PQR530 PI3K/mTOR inhibitor reduce huntingtin levels in cell models of HD.
Singer E; Walter C; Fabbro D; Rageot D; Beaufils F; Wymann MP; Rischert N; Riess O; Hillmann P; Nguyen HP
Neuropharmacology; 2020 Jan; 162():107812. PubMed ID: 31622602
[TBL] [Abstract][Full Text] [Related]
9. 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.
Beaufils F; Cmiljanovic N; Cmiljanovic V; Bohnacker T; Melone A; Marone R; Jackson E; Zhang X; Sele A; Borsari C; Mestan J; Hebeisen P; Hillmann P; Giese B; Zvelebil M; Fabbro D; Williams RL; Rageot D; Wymann MP
J Med Chem; 2017 Sep; 60(17):7524-7538. PubMed ID: 28829592
[TBL] [Abstract][Full Text] [Related]
10. Rapamycin passes the torch: a new generation of mTOR inhibitors.
Benjamin D; Colombi M; Moroni C; Hall MN
Nat Rev Drug Discov; 2011 Oct; 10(11):868-80. PubMed ID: 22037041
[TBL] [Abstract][Full Text] [Related]
11. A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor.
Borsari C; Rageot D; Dall'Asen A; Bohnacker T; Melone A; Sele AM; Jackson E; Langlois JB; Beaufils F; Hebeisen P; Fabbro D; Hillmann P; Wymann MP
J Med Chem; 2019 Sep; 62(18):8609-8630. PubMed ID: 31465220
[TBL] [Abstract][Full Text] [Related]
12. Discovery of 3,6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3,4-d]pyrimidines and 2-arylthieno[3,2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).
Kaplan J; Verheijen JC; Brooijmans N; Toral-Barza L; Hollander I; Yu K; Zask A
Bioorg Med Chem Lett; 2010 Jan; 20(2):640-3. PubMed ID: 19963384
[TBL] [Abstract][Full Text] [Related]
13. Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015-2021).
Oleksak P; Nepovimova E; Chrienova Z; Musilek K; Patocka J; Kuca K
Eur J Med Chem; 2022 Aug; 238():114498. PubMed ID: 35688004
[TBL] [Abstract][Full Text] [Related]
14. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin.
Yu K; Toral-Barza L; Shi C; Zhang WG; Lucas J; Shor B; Kim J; Verheijen J; Curran K; Malwitz DJ; Cole DC; Ellingboe J; Ayral-Kaloustian S; Mansour TS; Gibbons JJ; Abraham RT; Nowak P; Zask A
Cancer Res; 2009 Aug; 69(15):6232-40. PubMed ID: 19584280
[TBL] [Abstract][Full Text] [Related]
15. The novel, catalytic mTORC1/2 inhibitor PQR620 and the PI3K/mTORC1/2 inhibitor PQR530 effectively cross the blood-brain barrier and increase seizure threshold in a mouse model of chronic epilepsy.
Brandt C; Hillmann P; Noack A; Römermann K; Öhler LA; Rageot D; Beaufils F; Melone A; Sele AM; Wymann MP; Fabbro D; Löscher W
Neuropharmacology; 2018 Sep; 140():107-120. PubMed ID: 30081001
[TBL] [Abstract][Full Text] [Related]
16. Inhibition of 4EBP phosphorylation mediates the cytotoxic effect of mechanistic target of rapamycin kinase inhibitors in aggressive B-cell lymphomas.
Bi C; Zhang X; Lu T; Zhang X; Wang X; Meng B; Zhang H; Wang P; Vose JM; Chan WC; McKeithan TW; Fu K
Haematologica; 2017 Apr; 102(4):755-764. PubMed ID: 28104700
[TBL] [Abstract][Full Text] [Related]
17. Design, synthesis and biological evaluation of novel 9-methyl-9H-purine and thieno[3, 2-d]pyrimidine derivatives as potent mTOR inhibitors.
Yang YY; Wang WL; Hu XT; Chen X; Ni Y; Lei YH; Qiu QY; Tao LY; Luo TW; Wang NY
Bioorg Chem; 2023 Mar; 132():106356. PubMed ID: 36669357
[TBL] [Abstract][Full Text] [Related]
18. Catalytic mammalian target of rapamycin inhibitors as antineoplastic agents.
Mohindra NA; Platanias LC
Leuk Lymphoma; 2015; 56(9):2518-23. PubMed ID: 25747970
[TBL] [Abstract][Full Text] [Related]
19. Furthering the design and the discovery of small molecule ATP-competitive mTOR inhibitors as an effective cancer treatment.
Lv X; Ma X; Hu Y
Expert Opin Drug Discov; 2013 Aug; 8(8):991-1012. PubMed ID: 23668243
[TBL] [Abstract][Full Text] [Related]
20. Overview of Research into mTOR Inhibitors.
Mao B; Zhang Q; Ma L; Zhao DS; Zhao P; Yan P
Molecules; 2022 Aug; 27(16):. PubMed ID: 36014530
[TBL] [Abstract][Full Text] [Related]
[Next] [New Search]
