LINKS TO SCIENTIFIC PLATFORMS
https://orcid.org/0000-0002-4688-8362
https://publons.com/researcher/3510286/chiara-borsari/
https://scholar.google.com/citations?user=35muV-sAAAAJ&hl=en
https://www.scopus.com/authid/detail.uri?authorId=57113518800
PUBLICATIONS IN INTERNATIONAL PEER-REVIEWED SCIENTIFIC JOURNALS
Borsari C and Wymann MP. Targeting Phosphoinositide 3-Kinase – Five Decades of Chemical Space Exploration. CHIMIA. 2021 (accepted paper)
Magoulas GE, Afroudakis P, Georgikopoulou K, Roussaki M, Borsari C, Fotopoulou T, Santarem N, Barrias E, Tejera Nevado P, Hachenberg J, Bifeld E, Ellinger B, Kuzikov M, Fragiadaki I, Scoulica E, Clos J, Gul S, Costi MP, de Souza W, Prousis KC, Cordeiro da Silva A, Calogeropoulou T. Design, Synthesis and Antiparasitic Evaluation of Click Phospholipids. Molecules. 2021, 26 (14), 4204. doi: 10.3390/molecules26144204
Borsari C, De Pascale M, Wymann MP. Chemical and Structural Strategies to Selectively Target mTOR Kinase. ChemMedChem. 2021, 16 (18), 2744-2759. doi: 10.1002/cmdc.202100332 Invitation in EuroMedChemTalents Special Collection.
Borsari C, Keles E, Treyer A, De Pascale M, Hebeisen P, Hamburger M, Wymann MP. Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood–brain barrier permeability. RSC Med. Chem.2021,12 (4), 579-583. doi: 10.1039/D0MD00408A
Rathinaswamy MK, Gaieb Z, Fleming KD, Borsari C, Harris NJ, Moeller BE, Wymann MP, Amaro RE, Burke JE. Disease-related mutations in PI3Kγ disrupt regulatory C-terminal dynamics and reveal a path to selective inhibitors. Elife. 2021, 10, e64691. doi: 10.7554/eLife.64691
Borsari C, Keles E, Rageot D, De Pascale M, Treyer A, Bohnacker T, Melone A, Sriramaratnam R, Beaufils F, Hamburger M, Hebeisen P, Löscher W, Fabbro D, Hillmann P, Wymann MP. 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 Disorders. J Med Chem.2020, 63 (22), 13595-13617. doi: 10.1021/acs.jmedchem.0c00620
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. Identification of a 2,4-Diaminopyrimidine Scaffold Targeting Trypanosoma brucei Pteridine Reductase 1 from the LIBRA Compound Library Screening Campaign. Eur J Med Chem.2020, 189, 112047. doi: 10.1016/j.ejmech.2020.112047
Franchini S, Linciano P, Puja G, Tait A, Borsari C, Denora N, Iacobazzi RM, Brasili L, Sorbi C. Novel Dithiolane-Based Ligands Combining Sigma and NMDA Receptor Interactions as Potential Neuroprotective Agents. ACS Med Chem Lett.2020, 11 (5), 1028-1034. doi: 10.1021/acsmedchemlett.0c00129
Borsari C, Trader DJ, Tait A, Costi MP. Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology.J Med Chem. 2020, 63 (5), 1908-1928. doi: 10.1021/acs.jmedchem.9b01456
Borsari C, Rageot D, Beaufils F, Bohnacker T, Keles E, Buslov I, Melone A, Sele AM, Hebeisen P, Fabbro D, Hillmann P, Wymann MP. Preclinical Development of PQR514, a Highly Potent PI3K Inhibitor Bearing a Difluoromethyl-Pyrimidine Moiety. ACS Med Chem Letters2019, 10 (10), 1473-1479. doi: 10.1021/acsmedchemlett.9b00333
Rageot D, Beaufils F, Borsari C, Dall’Asen A, Neuburger M, Hebeisen P, Wymann MP. A Scalable, Economical and Safe Synthesis of 4-(Difluoromethyl)pyridin-2-amine, a Key Intermediate for Lipid Kinase Inhibitors. Org. Process Res. Dev.2019, 23, 11, 2416-2424. doi: 10.1021/acs.oprd.9b00312
Borsari C, Rageot D, Dall'Asen A, Bohnacker T, Melone A, Sele AM, Jackson E, Langlois JB, Beaufils F, Hebeisen P, Fabbro D, Hillmann P, Wymann MP. A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-Pyrrolo-Oxazine mTOR Inhibitor. J Med Chem.2019, 62 (18), 8609-8630.doi: 10.1021/acs.jmedchem.9b00972
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. (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. J Med Chem.2019, 62 (13), 6241-6261. doi: 10.1021/acs.jmedchem.9b00525
Borsari C, Jiménez-Antón MD, Eick J, Bifeld E, Torrado JJ, Olías-Molero AI, Corral MJ, Santarem N, Baptista C, Severi L, Gul S, Wolf M, Kuzikov M, Ellinger B, Reinshagen J, Witt G, Linciano P, Tait A, Costantino L, Luciani R, Tejera Nevado P, Zander-Dinse D, Franco CH, Ferrari S, Moraes CB, Cordeiro-da-Silva A, Ponterini G, Clos J, Alunda JM, Costi MP. Discovery of a Benzothiophene-flavonol Halting Miltefosine and Antimonial Drug Resistance in Leishmania Parasites Through the Application of Medicinal Chemistry, Screening and Genomics. Eur J Med Chem. 2019, 183, 111676.doi: 10.1016/j.ejmech.2019.111676
Landi G, Linciano P, Borsari C, Bertolacini CP, Moraes CB, Cordeiro-da-Silva A, Gul S, Witt G, Kuzikov M, Costi MP, Pozzi C, Mangani S. Structural Insights into the Development of Cycloguanil Derivatives as Trypanosoma brucei Pteridine Reductase 1 Inhibitors. ACS Infect. Dis.2019, 5 (7), 1105-1114. doi: 10.1021/acsinfecdis.8b00358
Borsari C, Santarem N, Macedo S, Jiménez-Antón MD, Torrado JJ, Olías-Molero AI, Corral MJ, Tait A, Ferrari S, Costantino L, Luciani R, Ponterini G, Gul S, Kuzikov M, Ellinger B, Behrens B, Reinshagen J, Alunda JM, Cordeiro-da-Silva A, Costi MP. SAR Studies and Biological Characterization of a Chromen-4-one Derivative as an Anti-Trypanosoma brucei Agent. ACS Med Chem Letters.2019, 10 (4), 528-533. doi: 10.1021/acsmedchemlett.8b00565
Vanossi D, Caselli M, Pavesi G, Borsari C, Linciano P, Costi MP, Ponterini G. Excited-state Intramolecular Proton Transfer in a Bioactive Flavonoid Provides Fluorescence Observables for Recognizing its Engagement with Target Proteins.Photochem Photobiol Sci.2019, 18, 2270-2280. doi: 10.1039/c9pp00026g
Moraes CB, Witt G, Kuzikov M, Ellinger B, Calogeropoulou T, Prousis KC, Mangani S, Di Pisa F, Landi G, Iacono LD, Pozzi C, Freitas-Junior LH, Dos Santos Pascoalino B, Bertolacini CP, Behrens B, Keminer O, Leu J, Wolf M, Reinshagen J, Cordeiro-da-Silva A, Santarem N, Venturelli A, Wrigley S, Karunakaran D, Kebede B, Pöhner I, Müller W, Panecka-Hofman J, Wade RC, Fenske M, Clos J, Alunda JM, Corral MJ, Uliassi E, Bolognesi ML, Linciano P, Quotadamo A, Ferrari S, Santucci M, Borsari C, Costi MP, Gul S. Accelerating Drug Discovery Efforts for Trypanosomatidic Infections Using an Integrated Transnational Academic Drug Discovery Platform. SLAS Discovery. 2019, 24 (3), 346-361. doi: 10.1177/2472555218823171
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. 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. J Med Chem.2018, 61 (22), 10084-10105.doi: 10.1021/acs.jmedchem.8b01262
Uliassi E, Piazzi L, Belluti F, Mazzanti A, Kaiser M, Brun R, Moraes CB, Freitas-Junior LH, Gul S, Kuzikov M, Ellinger B, Borsari C, Costi MP, Bolognesi ML. Development of a Focused Library of Triazole-Linked Privileged-Structure-Based Conjugates Leading to the Discovery of Novel Phenotypic Hits against Protozoan Parasitic Infections.ChemMedChem.2018, 13 (7), 678-683. doi: 10.1002/cmdc.201700786
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. 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.J Med Chem.2017, 60 (17), 7524-7538. doi: 10.1021/acs.jmedchem.7b00930
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. Crassiflorone Derivatives that Inhibit Trypanosoma brucei Glyceraldehyde-3-phosphate Dehydrogenase (TbGAPDH) and Trypanosoma cruzi Trypanothione Reductase (TcTR) and Display Trypanocidal Activity.Eur J Med Chem. 2017, 141, 138-148. doi: 10.1016/j.ejmech.2017.10.005
Di Pisa, F Landi G, Dello Iacono L, Pozzi C, Borsari C, Ferrari S, Santucci M, Santarem N, Cordeiro-da-Silva A, Moraes CB, Alcantara LM, Fontana V, Freitas-Junior LH, Gul S, Kuzikov M, Behrens B, Pöhner I, Wade RC, Costi MP, Mangani S. Chroman-4-One Derivatives Targeting Pteridine Reductase 1 and Showing Anti-Parasitic Activity.Molecules.2017, 22 (3), E426. doi: 10.3390/molecules22030426
Borsari C, Santarem N, Torrado J, Olías AI, Corral MJ, Baptista C, Gul S, Wolf M, Kuzikov M, Ellinger B, Witt G, Gribbon P, Reinshagen J, Linciano P, Tait A, Costantino L, Freitas-Junior LH, Moraes CB, Bruno Dos Santos P, Alcântara LM, Franco CH, Bertolacini CD, Fontana V, Tejera Nevado P, Clos J, Alunda JM, Cordeiro-da-Silva A, Ferrari S, Costi MP. Methoxylated 2'-Hydroxychalcones as Antiparasitic Hit Compounds. Eur J Med Chem. 2017, 126, 1129-1135. doi: 10.1016/j.ejmech.2016.12.017
Borsari C, Ferrari S, Venturelli A, Costi MP. Target-based Approaches for the Discovery of New Antimycobacterial Drugs.Drug Discov Today.2017, 22, (3), 576-584. doi: 10.1016/j.drudis.2016.11.014
Luciani R, Saxena P, Surade S, Santucci M, Venturelli A, Borsari C, Marverti G, Ponterini G, Ferrari S, Blundell TL, Costi MP. Virtual Screening and X-ray Crystallography Identify Non-Substrate Analog Inhibitors of Flavin-Dependent Thymidylate Synthase.J Med Chem. 2016, 59 (19), 9269-9275. doi: 10.1021/acs.jmedchem.6b00977
Catalano A, Luciani R, Carocci A, Cortesi D, Pozzi C, Borsari C, Ferrari S, Mangani S. X-ray Crystal Structures of Enterococcus faecalis Thymidylate Synthase with Folate Binding Site Inhibitors.Eur J Med Chem.2016, 123, 649-64. doi: 10.1016/j.ejmech.2016.07.066
Borsari C, Luciani R, Pozzi C, Poehner I, Henrich S, Trande M, Cordeiro-da-Silva A, Santarem N, Baptista C, Tait A, Di Pisa F, Dello Iacono L, Landi G, Gul S, Wolf M, Kuzikov M, Ellinger B, Reinshagen J, Witt G, Gribbon P, Kohler M, Keminer O, Behrens B, Costantino L, Tejera Nevado P, Bifeld E, Eick J, Clos J, Torrado J, Jiménez-Antón MD, Corral MJ, Alunda JM, Pellati F, Wade RC, Ferrari S, Mangani S, Costi MP. Profiling of Flavonol Derivatives for the Development of Anti-Trypanosomatidic Drugs.J Med Chem.2016, 59 (16), 7598-616. doi: 10.1021/acs.jmedchem.6b00698
Siragusa L, Luciani R, Borsari C, Ferrari S, Costi MP, Cruciani G, Spyrakis F. Comparing Drug Images and Repurposing Drugs with BioGPS and FLAPdock: The Thymidylate Synthase Case.ChemMedChem.2016, 11 (15), 1653-66. doi: 10.1002/cmdc.201600121
Franchini S, Battisti UM, Prandi A, Tait A, Borsari C, Cichero E, Fossa P, Cilia A, Prezzavento O, Ronsisvalle S, Aricò G, Parenti C, Brasili L. Scouting New Sigma Receptor Ligands: Synthesis, Pharmacological Evaluation and Molecular Modeling of 1,3-Dioxolane-based Structures and Derivatives.Eur J Med Chem.2016, 112, 1-19. doi: 10.1016/j.ejmech.2016.01.059
PEER-REVIEWED BOOKS
Borsari C, Quotadamo A, Ferrari S, Venturelli A, Cordeiro-da-Silva A, Santarem N, Costi MP. Scaffolds and Biological Targets Avenue to Fight Against Drug Resistance in Leishmaniasis, Annual Reports in Medicinal Chemistry, Neglected Diseases: Extensive Space for Modern Drug Discovery, Volume 51, Elsevier, 2018. doi: 10.1016/bs.armc.2018.08.002
PATENTS AND LICENSES
Wymann MP, Keles E, Borsari C (2021) Method for identifying PI3 Kinase-alpha Inhibitors
Eur. Patent Appl. EP21167756. [Priority date: 2021-Apr-10]
Wymann MP, Keles E, Borsari C (2021) Triazine derivative as reversible and irreversible covalent inhibitors of PI3K. Eur. Patent Appl. EP21167750. [Priority date: 2021-Apr-09]
Wymann MP, Keles E, Borsari C (2021) Triazine derivative as covalent inhibitors of PI3K
Eur. Patent Appl. EP21167749. [Priority date: 2021-Apr-09]
Costi MP, Costantino L, Borsari C, Ferrari S, Alunda Rodriguez JM, Cordeiro-da-Silva A. Novel Molecules with Anti-Parasitic Activity. Italian Patent: 102017000028966.