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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. Beaufils F, et al. Among authors: hillmann p. J Med Chem. 2017 Sep 14;60(17):7524-7538. doi: 10.1021/acs.jmedchem.7b00930. Epub 2017 Sep 1. J Med Chem. 2017. PMID: 28829592 Free PMC article.
PQR309 Is a Novel Dual PI3K/mTOR Inhibitor with Preclinical Antitumor Activity in Lymphomas as a Single Agent and in Combination Therapy.
Tarantelli C, Gaudio E, Arribas AJ, Kwee I, Hillmann P, Rinaldi A, Cascione L, Spriano F, Bernasconi E, Guidetti F, Carrassa L, Pittau RB, Beaufils F, Ritschard R, Rageot D, Sele A, Dossena B, Rossi FM, Zucchetto A, Taborelli M, Gattei V, Rossi D, Stathis A, Stussi G, Broggini M, Wymann MP, Wicki A, Zucca E, Cmiljanovic V, Fabbro D, Bertoni F. Tarantelli C, et al. Among authors: hillmann p. Clin Cancer Res. 2018 Jan 1;24(1):120-129. doi: 10.1158/1078-0432.CCR-17-1041. Epub 2017 Oct 24. Clin Cancer Res. 2018. PMID: 29066507
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: hillmann p. 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.
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. Brandt C, et al. Among authors: hillmann p. Neuropharmacology. 2018 Sep 15;140:107-120. doi: 10.1016/j.neuropharm.2018.08.002. Epub 2018 Aug 3. Neuropharmacology. 2018. PMID: 30081001
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. Rageot D, et al. Among authors: hillmann p. J Med Chem. 2018 Nov 21;61(22):10084-10105. doi: 10.1021/acs.jmedchem.8b01262. Epub 2018 Nov 14. J Med Chem. 2018. PMID: 30359003 Free article.
The Novel TORC1/2 Kinase Inhibitor PQR620 Has Anti-Tumor Activity in Lymphomas as a Single Agent and in Combination with Venetoclax.
Tarantelli C, Gaudio E, Hillmann P, Spriano F, Sartori G, Aresu L, Cascione L, Rageot D, Kwee I, Beaufils F, Zucca E, Stathis A, Wymann MP, Cmiljanovic V, Fabbro D, Bertoni F. Tarantelli C, et al. Among authors: hillmann p. Cancers (Basel). 2019 Jun 4;11(6):775. doi: 10.3390/cancers11060775. Cancers (Basel). 2019. PMID: 31167506 Free PMC article.
(S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase.
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. Rageot D, et al. Among authors: hillmann p. J Med Chem. 2019 Jul 11;62(13):6241-6261. doi: 10.1021/acs.jmedchem.9b00525. Epub 2019 Jun 20. J Med Chem. 2019. PMID: 31244112 Free article.
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. Borsari C, et al. Among authors: hillmann p. J Med Chem. 2019 Sep 26;62(18):8609-8630. doi: 10.1021/acs.jmedchem.9b00972. Epub 2019 Sep 11. J Med Chem. 2019. PMID: 31465220 Free article.
24 results