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ACS Medicinal Chemistry Letters|October 18, 2019
Preclinical Development of PQR514, a Highly Potent PI3K Inhibitor Bearing a Difluoromethyl-Pyrimidine MoietyChiara Borsari, Denise Rageot, Florent Beaufils, et al.Neuropharmacology|August 7, 2018
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 epilepsyClaudia Brandt, Petra Hillmann, Andreas Noack, et al.Journal of Medicinal Chemistry|August 30, 2019
A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR InhibitorChiara Borsari, Denise Rageot, Alix Dall'Asen, et al.Journal of Medicinal Chemistry|October 26, 2018
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 DisordersDenise Rageot, Thomas Bohnacker, Anna Melone, et al.European Journal of Medicinal Chemistry|January 12, 2023
Investigation of morpholine isosters for the development of a potent, selective and metabolically stable mTOR kinase inhibitorMartina De Pascale, Lukas Bissegger, Chiara Tarantelli, et al.Cancers|June 7, 2019
The Novel TORC1/2 Kinase Inhibitor PQR620 Has Anti-Tumor Activity in Lymphomas as a Single Agent and in Combination with VenetoclaxChiara Tarantelli, Eugenio Gaudio, Petra Hillmann, et al.Journal of Medicinal Chemistry|November 9, 2020
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 DisordersChiara Borsari, Erhan Keles, Denise Rageot, et al.Journal of Medicinal Chemistry|June 28, 2019
(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 KinaseDenise Rageot, Thomas Bohnacker, Erhan Keles, et al.Journal of Medicinal Chemistry|August 23, 2017
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 OncologyFlorent Beaufils, Natasa Cmiljanovic, Vladimir Cmiljanovic, et al.Nature Communications|March 10, 2017
Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic interventionThomas Bohnacker, Andrea E Prota, Florent Beaufils, et al.Pageof 3