Anna Melone

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

Florent Beaufils, Nataša Cmiljanović, Vladimir Cmiljanović et al. · Journal of Medicinal Chemistry · 2017 · 132 citations · Full text

Chemoprevention Strategy, Immunology, Clinical Candidate +19

Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention

Thomas Bohnacker, A.E. Prota, Florent Beaufils et al. · Nature Communications · 2017 · 113 citations · Full text

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

Denise Rageot, Thomas Bohnacker, Anna Melone et al. · Journal of Medicinal Chemistry · 2018 · 83 citations · Full text

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

Claudia Brandt, Petra Hillmann, Andreas Noack et al. · Neuropharmacology · 2018 · 79 citations

Chronic Epilepsy, Medicine, Pi3k/mtorc1/2 Inhibitor Pqr530 +7

(<i>S</i>)-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

Denise Rageot, Thomas Bohnacker, Erhan Keleş et al. · Journal of Medicinal Chemistry · 2019 · 54 citations · Full text

Compound 6, Brain Penetration, Cellular Pharmacology +25