| 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 … F Beaufils, N Cmiljanovic, V Cmiljanovic, T Bohnacker, A Melone, ... Journal of medicinal chemistry 60 (17), 7524-7538, 2017 | 122 | 2017 |
| 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 … D Rageot, T Bohnacker, A Melone, JB Langlois, C Borsari, P Hillmann, ... Journal of medicinal chemistry 61 (22), 10084-10105, 2018 | 71 | 2018 |
| (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 … D Rageot, T Bohnacker, E Keles, JA McPhail, RM Hoffmann, A Melone, ... Journal of medicinal chemistry 62 (13), 6241-6261, 2019 | 51 | 2019 |
| Profiling of flavonol derivatives for the development of antitrypanosomatidic drugs C Borsari, R Luciani, C Pozzi, I Poehner, S Henrich, M Trande, ... Journal of medicinal chemistry 59 (16), 7598-7616, 2016 | 50 | 2016 |
| Chroman-4-one derivatives targeting pteridine reductase 1 and showing anti-parasitic activity F Di Pisa, G Landi, L Dello Iacono, C Pozzi, C Borsari, S Ferrari, ... Molecules 22 (3), 426, 2017 | 47 | 2017 |
| Designing chimeric molecules for drug discovery by leveraging chemical biology C Borsari, DJ Trader, A Tait, MP Costi Journal of medicinal chemistry 63 (5), 1908-1928, 2020 | 43 | 2020 |
| Target-based approaches for the discovery of new antimycobacterial drugs C Borsari, S Ferrari, A Venturelli, MP Costi Drug Discovery Today 22 (3), 576-584, 2017 | 37 | 2017 |
| Crassiflorone derivatives that inhibit Trypanosoma brucei glyceraldehyde-3-phosphate dehydrogenase (TbGAPDH) and Trypanosoma cruzi trypanothione reductase (TcTR) and display … E Uliassi, G Fiorani, RL Krauth-Siegel, C Bergamini, R Fato, G Bianchini, ... European Journal of Medicinal Chemistry 141, 138-148, 2017 | 32 | 2017 |
| Covalent proximity scanning of a distal cysteine to target PI3Kα C Borsari, E Keles, JA McPhail, A Schaefer, R Sriramaratnam, W Goch, ... Journal of the American Chemical Society 144 (14), 6326-6342, 2022 | 31 | 2022 |
| Preclinical development of PQR514, a highly potent PI3K inhibitor bearing a Difluoromethyl–Pyrimidine moiety C Borsari, D Rageot, F Beaufils, T Bohnacker, E Keles, I Buslov, A Melone, ... ACS medicinal chemistry letters 10 (10), 1473-1479, 2019 | 31 | 2019 |
| Scouting new sigma receptor ligands: Synthesis, pharmacological evaluation and molecular modeling of 1, 3-dioxolane-based structures and derivatives S Franchini, UM Battisti, A Prandi, A Tait, C Borsari, E Cichero, P Fossa, ... European Journal of Medicinal Chemistry 112, 1-19, 2016 | 30 | 2016 |
| A conformational restriction strategy for the identification of a highly selective pyrimido-pyrrolo-oxazine mTOR inhibitor C Borsari, D Rageot, A Dall’Asen, T Bohnacker, A Melone, AM Sele, ... Journal of medicinal chemistry 62 (18), 8609-8630, 2019 | 28 | 2019 |
| Methoxylated 2'-hydroxychalcones as antiparasitic hit compounds C Borsari, N Santarem, J Torrado, AI Olías, MJ Corral, C Baptista, S Gul, ... European Journal of Medicinal Chemistry 126, 1129-1135, 2017 | 26 | 2017 |
| Disease related mutations in PI3Kγ disrupt regulatory C-terminal dynamics and reveal a path to selective inhibitors MK Rathinaswamy, Z Gaieb, KD Fleming, C Borsari, NJ Harris, BJ Moeller, ... Elife 10, e64691, 2021 | 25 | 2021 |
| Discovery of a benzothiophene-flavonol halting miltefosine and antimonial drug resistance in Leishmania parasites through the application of medicinal chemistry, screening and … C Borsari, MD Jiménez-Antón, J Eick, E Bifeld, JJ Torrado, ... European Journal of Medicinal Chemistry 183, 111676, 2019 | 22 | 2019 |
| Accelerating drug discovery efforts for trypanosomatidic infections using an integrated transnational academic drug discovery platform CB Moraes, G Witt, M Kuzikov, B Ellinger, T Calogeropoulou, KC Prousis, ... SLAS DISCOVERY: Advancing Life Sciences R&D 24 (3), 346-361, 2019 | 22 | 2019 |
| Virtual screening and X-ray crystallography identify non-substrate analog inhibitors of flavin-dependent thymidylate synthase R Luciani, P Saxena, S Surade, M Santucci, A Venturelli, C Borsari, ... Journal of Medicinal Chemistry 59 (19), 9269-9275, 2016 | 21 | 2016 |
| Comparing drug images and repurposing drugs with BioGPS and FLAPdock: the thymidylate synthase case L Siragusa, R Luciani, C Borsari, S Ferrari, MP Costi, G Cruciani, ... ChemMedChem 11 (15), 1653-1666, 2016 | 21 | 2016 |
| X-ray crystal structures of Enterococcus faecalis thymidylate synthase with folate binding site inhibitors A Catalano, R Luciani, A Carocci, D Cortesi, C Pozzi, C Borsari, S Ferrari, ... European Journal of Medicinal Chemistry 123, 649-664, 2016 | 19 | 2016 |
| 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 … C Borsari, E Keles, D Rageot, A Treyer, T Bohnacker, L Bissegger, ... Journal of medicinal chemistry 63 (22), 13595-13617, 2020 | 18 | 2020 |
Matthias P. WymannDepartment of Biomedicine, University of Basel, SwitzerlandVerified email at UniBas.CH
