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Chiara Borsari
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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 …
F Beaufils, N Cmiljanovic, V Cmiljanovic, T Bohnacker, A Melone, ...
Journal of medicinal chemistry 60 (17), 7524-7538, 2017
1262017
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
742018
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
562016
(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
552019
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
532017
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
502020
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
422022
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
392017
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
352017
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
342019
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
342019
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, ...
Elife 10, e64691, 2021
302021
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
302017
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
302016
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
262019
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
242019
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
232016
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
222016
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
212016
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
202020
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