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Identification of a 2,4-diaminopyrimidine scaffold targeting Trypanosoma brucei pteridine reductase 1 from the LIBRA compound library screening campaign.
Linciano P, Cullia G, Borsari C, Santucci M, Ferrari S, Witt G, Gul S, Kuzikov M, Ellinger B, Santarém N, Cordeiro da Silva A, Conti P, Bolognesi ML, Roberti M, Prati F, Bartoccini F, Retini M, Piersanti G, Cavalli A, Goldoni L, Bertozzi SM, Bertozzi F, Brambilla E, Rizzo V, Piomelli D, Pinto A, Bandiera T, Costi MP. Linciano P, et al. Among authors: borsari c. Eur J Med Chem. 2020 Mar 1;189:112047. doi: 10.1016/j.ejmech.2020.112047. Epub 2020 Jan 10. Eur J Med Chem. 2020. PMID: 31982652 Free article.
Discovery of 1,3,4-Oxadiazole Derivatives as Broad-Spectrum Antiparasitic Agents.
Corfu AI, Santarem N, Luelmo S, Mazza G, Greco A, Altomare A, Ferrario G, Nasta G, Keminer O, Aldini G, Tamborini L, Basilico N, Parapini S, Gul S, Cordeiro-da-Silva A, Conti P, Borsari C. Corfu AI, et al. Among authors: borsari c. ACS Infect Dis. 2024 May 8. doi: 10.1021/acsinfecdis.4c00181. Online ahead of print. ACS Infect Dis. 2024. PMID: 38717116
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: borsari c. 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.
Crassiflorone derivatives that inhibit Trypanosoma brucei glyceraldehyde-3-phosphate dehydrogenase (TbGAPDH) and Trypanosoma cruzi trypanothione reductase (TcTR) and display trypanocidal activity.
Uliassi E, Fiorani G, Krauth-Siegel RL, Bergamini C, Fato R, Bianchini G, Carlos Menéndez J, Molina MT, López-Montero E, Falchi F, Cavalli A, Gul S, Kuzikov M, Ellinger B, Witt G, Moraes CB, Freitas-Junior LH, Borsari C, Costi MP, Bolognesi ML. Uliassi E, et al. Among authors: borsari c. Eur J Med Chem. 2017 Dec 1;141:138-148. doi: 10.1016/j.ejmech.2017.10.005. Epub 2017 Oct 3. Eur J Med Chem. 2017. PMID: 29031061
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: borsari c. 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.
(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: borsari c. 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.
46 results