Publications

Vicinanza S, Mombelli L, Annunziata F, Donzella S, Contente ML, Borsari C, Conti P, Meroni G, Molinari F, Martino PA, Pinto A, Tamborini L. Chemo-enzymatic flow synthesis of nature-inspired phenolic carbonates and carbamates as antiradical and antimicrobial agents. Sustain Chem Pharm. 2024, 39, 101542.

DOI: 10.1016/j.scp.2024.101542

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Pollon D, Annunziata F, Paganelli S, Tamborini L, Pinto A, Fabris S, Baldo MA, Piccolo O. Improved Process for the Continuous Acylation of 1,3-Benzodioxole. Molecules 2024, 29, 726.

DOI: 10.3390/molecules29030726.

Galbiati A, Bova S, Pacchiana R, Borsari C, Persico M, Zana A, Bruno S, Donadelli M, Fattorusso C, Conti P. Discovery of a spirocyclic 3-bromo-4,5-dihydroisoxazole covalent inhibitor of hGAPDH with antiproliferative activity against pancreatic cancer cells. Eur J Med Chem. 2023, 254, 115286.

DOI: 10.1016/j.ejmech.2023.115286.

De Pascale M, Bissegger L, Tarantelli C, Beaufils F, Prescimone A, Mohamed Seid Hedad H, Kayali O, Orbegozo C, Raguž L, Schaefer T, Hebeisen P, Bertoni F, Wymann MP, Borsari C. Investigation of morpholine isosters for the development of a potent, selective and metabolically stable mTOR kinase inhibitor. Eur J Med Chem. 2023, 248, 115038.

DOI: 10.1016/j.ejmech.2022.115038.

Vicinanza S, Annunziata F, Pecora D, Pinto A, Tamborini L. Lipase-mediated flow synthesis of nature-inspired phenolic carbonates. RCS Adv. 2023, 13, 22901-22904. 

DOI: 10.1039/D3RA04735K.

Uros Stojiljkovic U, Meyer C, Boulay P, Hebeisen P, Rageot D, Wymann MP, Borsari C. Stereospecific Synthesis of Substituted Sulfamidates as Privileged Morpholine Building Blocks. Synthesis. 2023, 55 (03), 499-509.

DOI: 10.1055/a-1915-7794.

Colacicco A, Catinella G, Pinna C, Pellis A, Farris S, Zana A, Tamborini L, Dallavalle S, Molonari F, Contente M.L, Pinto A. Flow bioprocessing of citrus glycosides for high-value aglycone preparation. Catal. Sci. Technology. 2023, 13, 4348.

DOI: 10.1039/D3CY00603D.

Galbiati A, Zana A, Borsari C, Persico M, Bova S, Tkachuk O, Corfu I.A, Tamborini L, Basilico N, Fattorusso C, Bruno S, Parapini S, Conti P. Role of Stereochemistry on the Biological Activity of Nature-Inspired 3-Br-Acivicin Isomers and Derivatives. Molecules 2023, 28, 3172.

DOI:  10.3390/molecules28073172.

Ferrins L, Olson ME, Haranahalli K, Grenier-Davies MC, Boudreau MW, Matagne B, Donckele EJ, Borsari C. YMCC and YSN: An Opportunity for Scientific and Cultural Exchange.

ACS Med Chem Lett. 2023, 14, 1129-1130. DOI: 10.1021/acsmedchemlett.3c00337.

J Med Chem. 2023, 66 (17), 11591-11592. DOI: 10.1021/acs.jmedchem.3c01401.

Borsari C, Keles E, McPhail JA, Schaefer A, Sriramaratnam R, Goch W, Schaefer T, De Pascale M, Bal W, Gstaiger M, Burke JE, Wymann MP. Covalent Proximity Scanning of a Distal Cysteine to Target PI3Kα. J Am Chem Soc. 2022, 144 (14), 6326-6342.

DOI: 10.1021/jacs.1c13568.

Annunziata F, Guaglio A, Conti P, Tamborini L, Gandolfi R. Continuous-flow stereoselective reduction of prochiral ketones in a whole cell bioreactor with natural deep eutectic solvents. Green Chem. 2022, 24, 950-956.

DOI: 10.1039/D1GC03786B.

Pecora D, Annunziata F, Pegurri S, Picone P, Pinto A, Nuzzo D, Tamborini L. Flow Synthesis of Nature-Inspired Mitochondria-Targeted Phenolic Derivatives as Potential Neuroprotective Agents. Antioxidants (Basel). 2022, 11 (11), 2160.

DOI: 10.3390/antiox11112160.

Robescu MS, Annunziata F, Somma V, Calvio C, Morelli CF, Speranza G, Tamborini L, Ubiali D, Pinto A, Bavaro T. From Batch to Continuous Flow Bioprocessing: Use of an Immobilized γ-Glutamyl Transferase from B. subtilis for the Synthesis of Biologically Active Peptide Derivatives. J Agric Food Chem. 2022, 70 (42), 13692-13699.

DOI: 10.1021/acs.jafc.2c03702.

Annunziata F, Contente ML, Anzi V, Donzella S, Conti P, Molinari F, Martino PA, Meroni G, Sora VM, Tamborini L, Pinto A. Enzymatic continuous-flow preparation of nature-inspired phenolic esters as antiradical and antimicrobial agents. Food Chem. 2022, 390, 133195.

DOI: 10.1016/j.foodchem.2022.133195.

Pinna C, Martino PA, Meroni G, Sora VM, Tamborini L, Dallavalle S, Contente ML, Pinto A. Biocatalyzed Synthesis of Vanillamides and Evaluation of Their Antimicrobial Activity. J Agric Food Chem. 2022, 70 (1), 223-228.

DOI: 10.1021/acs.jafc.1c06213.

Pacchiana R, Mullappilly N, Pinto A, Bova S, Forciniti S, Cullia G, Dalla Pozza E, Bottani E, Decimo I, Dando I, Bruno S, Conti P, Donadelli M. 3-Bromo-Isoxazoline Derivatives Inhibit GAPDH Enzyme in PDAC Cells Triggering Autophagy and Apoptotic Cell Death. Cancers (Basel). 2022, 14 (13), 3153.

DOI: 10.3390/cancers14133153.

Wymann MP, Borsari C. Two-drug trick to target the brain blocks toxicity in the body. Nature. 2022, 609 (7928), 681-683.

DOI: 10.1038/d41586-022-02892-5.

Galbiati A, Zana A, Coser C, Tamborini L, Basilico N, Parapini S, Taramelli D, Conti P. Development of Potent 3-Br-isoxazoline-Based Antimalarial and Antileishmanial Compounds. ACS Med Chem Lett. 2021, 12 (11), 1726-1732.

DOI: 10.1021/acsmedchemlett.1c00354.

Contente ML, Annunziata F, Cannazza P, Donzella S, Pinna C, Romano D, Tamborini L, Barbosa FG, Molinari F, Pinto A. Biocatalytic Approaches for an Efficient and Sustainable Preparation of Polyphenols and Their Derivatives. J Agric Food Chem. 2021, 69 (46), 13669-13681.

DOI: 10.1021/acs.jafc.1c05088.

Annunziata F, Contente ML, Pinna C, Tamborini L, Pinto A. Biocatalyzed Flow Oxidation of Tyrosol to Hydroxytyrosol and Efficient Production of Their Acetate Esters. Antioxidants (Basel). 2021, 10 (7), 1142.

DOI: 10.3390/antiox10071142.

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. 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.

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, Wymann MP. Chimia (Aarau). Targeting Phosphoinositide 3-Kinase – Five Decades of Chemical Space Exploration. 2021, 75 (12), 1037-1044.

DOI: 10.2533/chimia.2021.1037.

Annunziata F, Contente ML, Betti D, Pinna C, Molinari F, Tamborini L, Pinto, A. Efficient Chemo-Enzymatic Flow Synthesis of High Value Amides and Esters. Catalysts. 2020, 10 (8), 939.

DOI: 10.3390/catal10080939.

Borsari C, Keles E, Rageot D, Treyer A, Bohnacker T, Bissegger L, De Pascale M, Melone A, Sriramaratnam R, Beaufils F, Hamburger M, Hebeisen P, Löscher W, Fabbro D, Hillmann P, Wymann MP. 4-(Difluoromethyl)-5-(4-((3 R,5 S)-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.

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.

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.

Tamborini L, Previtali C, Annunziata F, Bavaro T, Terreni M, Calleri E, Rinaldi F, Pinto A, Speranza G, Ubiali D, Conti P. An Enzymatic Flow-Based Preparative Route to Vidarabine. Molecules. 2020, 25 (5), 1223.

DOI: 10.3390/molecules25051223.

Rinaldi F, Fernández-Lucas J, de la Fuente D, Zheng C, Bavaro T, Peters B, Massolini G, Annunziata F, Conti P, de la Mata I, Terreni M, Calleri E. Immobilized enzyme reactors based on nucleoside phosphorylases and 2′-deoxyribosyltransferase for the in-flow synthesis of pharmaceutically relevant nucleoside analogues. Bioresour Technol. 2020, 307, 123258.

DOI: 10.1016/j.biortech.2020.123258.

Galbiati A, Zana A, Conti P. Covalent inhibitors of GAPDH: From unspecific warheads to selective compounds. Eur J Med Chem. 2020, 207, 112740.

DOI: 10.1016/j.ejmech.2020.112740.

Annunziata F, Pinna C, Dallavalle S, Tamborini L, Pinto A. An Overview of Coumarin as a Versatile and Readily Accessible Scaffold with Broad-Ranging Biological Activities. Int J Mol Sci. 2020, 21 (13), 4618.

DOI: 10.3390/ijms21134618.

Li Z, Bavaro T, Tengattini S, Bernardini R, Mattei M, Annunziata F, Cole RB, Zheng C, Sollogoub M, Tamborini L, Terreni M, Zhang Y. Chemoenzymatic synthesis of arabinomannan (AM) glycoconjugates as potential vaccines for tuberculosis. Eur J Med Chem. 2020, 204, 112578.

DOI: 10.1016/j.ejmech.2020.112578.

Contente M.L, Dall’Oglio F , Annunziata F, Molinari F, Rabuffetti M, Romano D, Tamborini L, Dörte R, Pinto A. Stereoselective Reduction of Prochiral Cyclic 1,3‐Diketones Using Different Biocatalysts. Catalysis Letters. 2020, 150, 1176-1185.

DOI: 10.1007/s10562-019-03015-y.

Semproli R, Vaccaro G , Ferrandi E.E, Vanoni M, Bavaro T, Marrubini G, Annunziata F, Conti P. Use of Immobilized Amine Transaminase from Vibrio fluvialis under Flow Conditions for the Synthesis of (S)-1-(5-Fluoropyrimidin-2-yl)-ethanamine. ChemCatChem. 2020, 12, 1359-1367.

DOI: 10.1002/cctc.201902080.

Contente M.L, Tamborini L, Molinari F, Paradisi F. Aromas flow: eco-friendly, continuous, and scalable preparation of flavour esters. Journal of Flow Chemistry. 2020, 10, 235-240.

DOI: 10.1007/s41981-019-00063-8.

Cullia G, Bruno S, Parapini S, Margiotta M, Tamborini L, Pinto A, Galbiati A, Mozzarelli A, Persico M, Paladino A, Fattorusso C, Taramelli D, Conti P. Covalent Inhibitors of Plasmodium falciparum Glyceraldehyde 3-Phosphate Dehydrogenase with Antimalarial Activity in Vitro. ACS Med Chem Lett. 2019, 10 (4), 590-595.

DOI: 10.1021/acsmedchemlett.8b00592.

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.

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 Lett. 2019, 10 (4), 528-533.

DOI: 10.1021/acsmedchemlett.8b00565.

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 Lett. 2019, 10 (10), 1473-1479.

DOI: 10.1021/acsmedchemlett.9b00333.

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.

Oliva F, Bucci R, Tamborini L, Pieraccini S, Pinto A, Pellegrino S. Bicyclic Pyrrolidine-Isoxazoline γ Amino Acid: A Constrained Scaffold for Stabilizing α-Turn Conformation in Isolated Peptides. Front Chem. 2019, 7, 133.

DOI: 10.3389/fchem.2019.00133.

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 Discov. 2019, 24 (3), 346-361.

DOI: 10.1177/2472555218823171.

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 (9), 2270-2280.

DOI: 10.1039/c9pp00026g.

Dell’Omo G, Crescenti D, Vantaggiato C, Parravicini C, Borroni AP, Rizzi N, Garofalo M, Pinto A, Recordati C, Scanziani E, Bassi FD, Pruneri G, Conti P, Eberini I, Maggi A, Ciana P. Inhibition of SIRT1 deacetylase and p53 activation uncouples the anti-inflammatory and chemopreventive actions of NSAIDs. Br J Cancer. 2019, 120 (5), 537-546.

DOI: 10.1038/s41416-018-0372-7.

Contente M.L, Farris S, Tamborini L, Molinari F, Paradisi F. Flow-based enzymatic synthesis of melatonin and other high value tryptamine derivatives: a five-minute intensified process Green Chem. 2019, 21, 3263

DOI: 10.1039/c9gc01374a.