IFOM Experimental Therapeutics Program

Mario Varasi Patents & Publications

Patents

  1. Pasqualato, Sebastiano; Pasi, Maurizio; Amici, Raffaella; Varasi, Mario; Mercurio, Ciro; Sartori, Luca; Polo, Simona; Maspero, Elena; Faga`, Giovanni
    Hect e3 ligase inhibitors and uses thereof
    PCT Int. Appl. (2020), WO 2020245213 A1 20201210

  2. Varasi, Mario; Cappa, Anna; Vianello, Paola; Moretti, Loris; Sartori, Luca; Mercurio, Ciro
    Thieno[2,?3-?b]?pyrrole and thieno[3,?2-?b]?pyrrole derivatives as histone demethylase inhibitors and their preparation
    PCT Int. Appl. (2019), WO 2019034774 A1 20190221

  3. Varasi, Mario; Villa, Manuela; Trifiró, Paolo; Fancelli, Daniele; Mercurio, Ciro; Vianello, Paola; Sartori, Luca
    Oxime derivatives useful as inhibitors of histone demethylase KDM4C and their preparation
    PCT Int. Appl. (2017), WO 2017198785 A1 20171123.

  4. Vianello, Paola; Romussi, Alessia; Cappa, Anna; Trifiró, Paolo; Varasi, Mario; Sartori, Luca; Mercurio, Ciro
    Preparation of imidazol-2-ylthienopyrrole compounds as histone demethylase inhibitors
    PCT Int. Appl. (2017), WO 2017198780 A1 20171123.

  5. Vianello, Paola; Sartori, Luca;Varasi, Mario; Mercurio, Ciro; Zagarri, Elisa; Cappa, Anna; Romussi, Alessia; Villa, Manuela; Meroni, Giuseppe; Moretti, Loris
    Thienopyrroles as histone demethylase inhibitors
    PCT Int. Appl. (2016), WO2016034946 A2 20160310

  6. Varasi, Mario; Cappa, Anna; Fancelli, Daniele; Romussi, Alessia
    Compounds inhibiting the enzyme monopolar spindle 1 kinase, pharmaceutical compositions and uses there of
    PCT Int. Appl.(2016), WO 2016001077 A1 20160107.

  7. Vianello, Paola; Varasi, Mario; Mercurio, Ciro; Cappa, Anna; Meroni, Giuseppe Villa, Manuela; Mai, Antonello; Valente, Sergio
    Cyclopropylamine compounds as histone demethylase inhibitors
    PCT Int. Appl. (2015), WO 2015181380 A1 20151203.

  8. Varasi, Mario; Vianello, Paola; Thaler, Florian; Trifiro, Paolo; Mercurio, Ciro; Meroni, Giuseppe
    Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a
    PCT Int. Appl. (2014), WO 2014086790 A1 20140612.

  9. Amici, Raffaella; Colombo, Andrea; Courtney, Stephen Martin; Mercurio, Ciro; Montalbetti, Christian Aldo Georges Napoleon; Mortoni, Annalisa; Varasi, Mario
    Preparation of quinazoline derivatives with Hsp90 inhibitory activity for therapy
    PCT Int. Appl. (2013), WO 2013064919 A1 20130510.

  10. Varasi, Mario; Thaler, Florian; Amici, Raffaella; Abate, Agnese; Fulco, Maria Carmela; Minucci, Saverio; Mercurio, Ciro.
    Spirocyclic derivatives as histone deacetylase inhibitors U.S.
    Pat. Appl. Publ. (2012), US 20120258949 A1 20121011

  11. Minucci, Saverio; Pelicci, Pier Giuseppe; Mai, Antonello; Ballarini, Marco; Gargiulo, Gaetano; Massa, Silvio; Thaler, Florian; Pain, Gilles; Colombo, Andrea; Gagliardi, Stefania; Varasi, Mario; Ciro, Mercurio
    Preparation of N-hydroxy piperazinyl-phenyl-oxo-propenyl-phenyl-acrylamides and related compounds as histone deacetylase inhibitors U.S.
    Pat. Appl. Publ. (2012), US 20120115867 A1 20120510

  12. Disingrini, Teresa; Mantegani, Sergio; Varasi, Mario.
    Tricyclopyrazole derivatives as protein kinase modulators and their preparation and use in the treatment of protein kinase-mediated diseases.
    PCT Int. Appl. (2011), WO 2011067145 A1 20110609 AN 2011:720686

  13. Varasi, Mario; Thaler, Florian; Amici, Raffaella; Abate, Agnese; Fulco, Maria Carmela; Minucci, Saverio; Mercurio, Ciro.
    Preparation of oxospirochromane derivatives as histone deacetylase inhibitors.
    PCT Int. Appl. (2011), WO 2011045265 A2 20110421

  14. Fancelli, Daniele; Varasi, Mario; Plyte, Simon; Ballarini, Marco; Cappa, Anna; Carenzi, Giacomo; Minucci, Saverio; Pain, Gilles; Villa, Manuela.
    Preparation of acrylamido derivatives as inhibitors of the mitochondrial permeability transition.
    PCT Int. Appl. (2010), WO 2010049768 A1 20100506

  15. Thaler, Florian; Varasi, Mario; Gagliardi, Stefania; Colombo, Andrea; Minucci, Saverio; Mercurio, Ciro.
    Heterocyclic derivatives as HDAC inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases.
    PCT Int. Appl. (2009), 98pp. WO 2009150129 A1 20091217

  16. Varasi, Mario; Thaler, Florian; Abate, Agnese; Carenzi, Giacomo; Minucci, Saverio.
    Preparation of oxospirochromanepiperidine derivatives and analogs for use as histone deacetylase inhibitors.
    PCT Int. Appl. (2009), WO 2009127609 A1 20091022

  17. Thaler, Florian; Varasi, Mario; Mercurio, Ciro; Minucci, Saverio; Colombo, Andrea; Gagliardi, Stefania.
    Preparation of N-hydroxy piperazinylphenyloxopropenylphenylacrylamides and related compounds as histone deacetylase inhibitors.
    PCT Int. Appl. (2009), WO 2009027395 A1 20090305

  18. Bandiera, Tiziano; Perrone, Ettore; Lombardi Borgia, Andrea; Varasi, Mario.
    Preparation of pyrazolo[4,3-c]pyridine derivatives as IGF-1R inhibitors.
    PCT Int. Appl. (2007), WO 2007099166 A1 20070907

  19. Vanotti, Ermes; Menichincheri, Maria; Orsini, Paolo; Scolaro, Alessandra; Varasi, Mario.
    Preparation of N-substituted pyrrolopyridinones active as kinase inhibitors.
    PCT Int. Appl. (2007) WO 2007068728 A2 20070621

Publications

  1. Zwergel, Clemens; Di Bello, Elisabetta; Fioravanti, Rossella; Conte, Mariarosaria; Nebbioso, Angela; Mazzone, Roberta; Brosch, Gerald; Mercurio, Ciro; Varasi, Mario; Altucci, Lucia; et al 1.
    Novel Pyridine-Based Hydroxamates and 2'-Aminoanilides as Histone Deacetylase Inhibitors: Biochemical Profile and Anticancer Activity
    ChemMedChem? (2021), 16(6), 989-999.

  2. Stefania Faletti; Daniela Osti; Elena Ceccacci; Cristina Richichi; Brunella Costanza; Luciano Nicosia; Roberta Noberini; Giulia Marotta; Laura Furia; Mario Faretta; Silvia Brambillasca; Micaela Quarto; Luca Bertero; Renzo Boldorini; Bianca Pollo; Sara Gandini; Davide Corà; Saverio Minucci; Ciro Mercurio; Mario Varasi; Tiziana Bonaldi; Giuliana Pelicci
    LSD1-directed therapy affects glioblastoma tumorigenicity by deregulating the protective ATF4-dependent integrated stress response
    Cell Stem Cell (Submitted)

  3. Francesca Cavallo, Flavia Troglio, Giovanni Fagà, Daniele Fancelli, Reinald Shyti, Sebastiano Trattaro, Matteo Zanella, Giuseppe D’Agostino, James M. Hughes, Maria Rosaria Cera, Maurizio Pasi, Michele Gabriele, Maddalena Lazzarin, Marija Mihailovich, Frank Kooy, Alessandro Rosa, Ciro Mercurio, Mario Varasi and Giuseppe Testa
    High-throughput screening identifies histone deacetylase inhibitors that modulate GTF2I expression in 7q11.23 microduplication autism spectrum disorder patient-derived cortical neurons
    Molecular Autism (2020), 11(1), 88

  4. Roberto Ravasio, Elena Ceccacci, Luciano Nicosia, Amir Hosseini, Pier Luigi Rossi, Iros Barozzi, Lorenzo Fornasari, Roberto Dal Zuffo, Sergio Valente, Rossella Fioravanti, Ciro Mercurio, Mario Varasi, Andrea Mattevi, Antonello Mai, Giulio Pavesi,Tiziana Bonaldi, Saverio Minucci
    Targeting the scaffolding role of LSD1 (KDM1A) poises acute myeloid leukemia cells for retinoicacid–induced differentiation
    Science advances (2020), 6(15), eaax2746

  5. Romussi, Alessia; Cappa, Anna; Vianello, Paola; Brambillasca, Silvia; Cera, Maria Rosaria; Dal Zuffo, Roberto; Faga`, Giovanni; Fattori, Raimondo; Moretti, Loris; Trifiro, Paolo; et al
    Discovery of Reversible Inhibitors of KDM1A Efficacious in Acute Myeloid Leukemia Models
    ACS Medicinal Chemistry Letters (2020), 11(5), 754-759.

  6. Ravasio, Roberto; Ceccacci, Elena; Nicosia, Luciano; Hosseini, Amir; Rossi, Pier Luigi; Barozzi, Iros; Fornasari, Lorenzo; Zuffo, Roberto Dal; Valente, Sergio; Fioravanti, Rossella; Mercurio, Ciro; Varasi, Mario; Mattevi, Andrea; Mai, Antonello; Pavesi, Giulio; Bonaldi, Tiziana; Minucci, Saverio
    Targeting the scaffolding role of LSD1 (KDM1A) poises acute myeloid leukemia cells for retinoic acid-?induced differentiation
    Science Advances (2020), 6(15), eaax2746.

  7. Paolo Trifiró, Anna Cappa, Oronza A. Botrugno, Roberto Dal Zuffo, Paola Dessanti, Giuseppe Meroni, Florian Thaler, Manuela Villa, Saverio Minucci, Ciro Mercurio, Mario Varasi, Paola Vianello
    Novel potent inhibitors of the histone demethylase KDM1A (LSD1), orally active in a murine promyelocitic leukemia model
    From Future Medicinal Chemistry (2017), 9(11), 1161-1174.

  8. Elisa Ferrari, Christopher Bruhn, Marta Peretti, Corinne Cassani, Walter Vincenzo Carotenuto, Mohamed Elgendy, Ghadeer Shubassi, Chiara Lucca, Rodrigo Bermejo, Mario Varasi, Saverio Minucci, Maria Pia Longhese, and Marco Foiani
    PP2A Controls Genome Integrity by Integrating Nutrient-Sensing and Metabolic Pathways with the DNA Damage Response
    Molecular Cell (2017), 67(2), 266-281.

  9. Luca Sartori, Ciro Mercurio, Federica Amigoni, Anna Cappa, Giovanni Fagà, Raimondo Fattori, Elena Legnaghi, Giuseppe Ciossani, Andrea Mattevi, Giuseppe Meroni, Loris Moretti, Valentina Cecatiello, Sebastiano Pasqualato, Alessia Romussi, Florian Thaler, Paolo Trifirò, Manuela Villa, Stefania Vultaggio, Oronza A. Botrugno, Paola Dessanti, Saverio Minucci, Elisa Zagarrì, Daniele Carettoni, Lucia Iuzzolino, Mario Varasi, Paola Vianello
    Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1.
    Part 1: High Throughput Screening and Preliminary Exploration (J.Med.Chem., 2017)

  10. Paola Vianello, Luca Sartori, Federica Amigoni, Anna Cappa, Giovanni Fagà, Raimondo Fattori, Elena Legnaghi, Giuseppe Ciossani, Andrea Mattevi, Giuseppe Meroni, Loris Moretti, Valentina Cecatiello, Sebastiano Pasqualato, Alessia Romussi,Florian Thaler, Paolo Trifirò, Manuela Villa, Oronza A. Botrugno, Paola Dessanti, Saverio Minucci, Stefania Vultaggio,Elisa Zagarrì, Mario Varasi, Ciro Mercurio
    Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1.
    Part 2: Structure Based Drug Design, SAR (J.Med.Chem., 2017)

  11. Paola Vianello,Oronza A. Botrugno, Anna Cappa, Roberto Dal Zuffo, Paola Dessanti, Antonello Mai, Andrea Mattevi, Giuseppe Meroni, Saverio Minucci, Florian Thaler, Paolo Trifirò, Sergio Valente, Manuela Villa, Mario Varasi and Ciro Mercurio
    Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent
    J.Med. Chem., (2016), 59(4), 1501-1517

  12. Florian Thaler, Loris Moretti, Raffaella Amici, Agnese Abate, Andrea Colombo, Giacomo Carenzi, Maria Carmela Fulco, Roberto Boggio, Giulio Dondio, Stefania Gagliardi, Saverio Minucci, Luca Sartori, Mario Varasi, and Ciro Mercurio
    Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors
    Eur.J.Med.Chem., (2016), 108, 53-67

  13. La Regina, Giuseppe; Bai, Ruoli; Coluccia, Antonio; Famiglini, Valeria; Pelliccia, Sveva; Passacantilli, Sara; Mazzoccoli, Carmela; Ruggieri, Vitalba; Verrico, Annalisa; Miele, Andrea; Monti, Ludovica; Nalli, Marianna; Alfonsi, Romina; Di Marcotullio, Lucia; Gulino, Alberto; Ricci, Biancamaria; Soriani, Alessandra; Santoni, Angela; Caraglia, Michele; Porto, Stefania; Da Pozzo, Eleonora; Martini, Claudia; Brancale, Andrea; Marinelli, Luciana; Novellino, Ettore; Vultaggio, Stefania; Varasi, Mario; Mercurio, Ciro; Bigogno, Chiara; Dondio, Giulio; Hamel, Ernest; Lavia, Patrizia; Silvestri, Romano
    New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity and Repression of Hedgehog-dependent Cancer
    Journal of Medicinal Chemistry (2015), 58 (15), 5789–5807

  14. Sergio Valente, Veronica Rodriguez, Ciro Mercurio, Paola Vianello, Bruna Saponara, Roberto Cirilli, Giuseppe Ciossani, Donatella Labella, Biagina Marrocco, Daria Monaldi, Giovanni Ruoppolo, Mats Tilset, Oronza A. Botrugno, Paola Dessanti, Saverio Minucci, Andrea Mattevi, Mario Varasi, and Antonello Mai
    Pure enantiomers of benzoylamino-tranylcypromine: LSD1 inhibition, gene modulation in human leukemia cells and effects on clonogenic potential of murine promyelocytic blasts
    European Journal of Medicinal Chemistry 4 (2015) 163-174

  15. Marco Pieroni, Giannamaria Annunziato, Elisa Azzali, Paola Dessanti, Ciro Mercurio, Giuseppe Meroni, Paolo Trifirò, Paola Vianello, Manuela Villa, Claudia Beato, Mario Varasi, and Gabriele Costantino
    Further Insights on the SAR of 1-Substituted Cyclopropylamine Derivatives as Inhibitors of Histone Demethylase LSD1
    European Journal of Medicinal Chemistry 92 (2015) 377-386

  16. Veronica Rodriguez, Sergio Valente, Giulia Stazi, Alessia Lucidi, Ciro Mercurio, Paola Vianello, Giuseppe Ciossani, Andrea Mattevi, Oronza A. Botrugno, Paola Dessanti, Saverio Minucci, Mario Varasi, and Antonello Mai
    Pyrrole- and indole-containing tranylcypromine derivatives as novel lysine-specific demethylase 1 inhibitors active on cancer cells
    MedChemComm, 6 (2015) 665-670

  17. Valente, Sergio; Rodriguez, Veronica; Mercurio, Ciro; Vianello, Paola; Saponara, Bruna; Cirilli, Roberto; Ciossani, Giuseppe; Labella, Donatella; Marrocco, Biagina; Ruoppolo, Giovanni; Botrugno, Oronza; Dessanti, Paola; Minucci, Saverio; Mattevi, Andrea; Varasi, Mario; Mai, Antonello
    Pure Diastereomers of a Tranylcypromine-based LSD1 Inhibitor: Enzyme Selectivity and In Cell Studies
    ACSMedChemLett, (2015), 6(2), 173-177

  18. Paola Vianello, Oronzina Botrugno, Anna Cappa, Giuseppe Ciossani, Paola Dessanti, Antonello Mai, Andrea Mattevi, Giuseppe Meroni, Saverio Minucci, Florian Thaler , Marcello Tortorici, Paolo Trifirò, Sergio Valente, Manuela Villa, Mario Varasi and Ciro Mercurio
    Synthesis, Biological Activity and Mechanistic Insights of 1-Substituted Cyclopropylamine Derivatives: a Novel Class of Irreversible Inhibitors of Histone Demethylases KDM1A
    European Journal of Medicinal Chemistry 86 (2014) 352-363

  19. La Regina, Giuseppe; Bai, Ruoli; Coluccia, Antonio; Famiglini, Valeria; Pelliccia, Sveva; Passacantilli, Sara; Mazzoccoli, Carmela; Ruggieri, Vitalba; Sisinni, Lorenza; Bolognesi, Alessio; Rensen, Whilelmina Maria; Miele, Andrea; Nalli, Marianna; Alfonsi, Romina; Di Marcotullio, Lucia; Gulino, Alberto; Brancale, Andrea; Novellino, Ettore; Dondio, Giulio; Vultaggio, Stefania; Varasi, Mario; Mercurio, Ciro; Hamel, Ernest; Lavia, Patrizia; Silvestri, Romano
    New Pyrrole Derivatives with Potent Tubulin Polymerization Inhibiting Activity as Anticancer Agents including Hedgehog-dependent Cancer
    Journal of Medicinal Chemistry (2014), 57 (15), 6531–6552

  20. Fancelli, Daniele; Abate, Agnese; Amici, Raffaella; Bernardi, Paolo; Ballarini, Marco; Cappa, Anna; Carenzi, Giacomo; Colombo, Andrea; Contursi, Cristina; Di Lisa, Fabio; Dondio, Giulio; Gagliardi, Stefania; Milanesi, Eva; Minucci, Saverio; Pain, Gilles; Pelicci, Pier Giuseppe; Saccani, Alessandra; Storto, Mariangela; Thaler, Florian; Varasi, Mario; Villa, Manuela; Plyte, Simon
    Cinnamic Anilides as New Mitochondrial Permeability Transition Pore Inhibitors Endowed with Ischemia-Reperfusion Injury Protective Effect in Vivo
    Journal of Medicinal Chemistry (2014), 57(12), 5333-5347

  21. Raffaella Amici, Chiara Bigogno, Roberto Boggio, Andrea Colombo, Stephen M. Courtney, Roberto Dal Zuffo, Giulio Dondio, Fulvia Fusar, Stefania Gagliardi, Saverio Minucci, Marco Molteni, Christian A. G. N. Montalbetti, Annalisa Mortoni, Mario Varasi,Stefania Vultaggio, and Ciro Mercurio
    The Chiral Resolution and Pharmacological Characterization of the Enantiomers of the Hsp90 Inhibitor 2-Amino-7-[4-fluoro-2-(3-pyridyl)phenyl]-4-methyl-7,8-dihydro-6h-quinazolin-5-one oxime
    ChemMedChem (2014), 9(7), 1574-1585

  22. Mara Colzani, Roberta Noberinia, Mauro Romanenghia, Gennaro Colellac, Maurizio Pasi, Daniele Fancellid, Mario Varasi, Saverio Minuccia, and Tiziana Bonaldi
    Quantitative chemical proteomics identifies novel targets of the anti-cancer multi-kinase inhibitor E-3810
    Molecular and Cellular Proteomics (2014), 13(6), 1495-1509

  23. Florian Thaler, Mario Varasi, Agnese Abate, Giacomo Carenzi, Andrea Colombo, Chiara Bigogno, Roberto Boggio, Roberto Dal Zuffo,Daniela Rapetti, Anna Resconi, Nickolas Regalia, Stefania Vultaggio, Giulio Dondio, Stefania Gagliardi, Saverio Minucci, Ciro Mercurio
    Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine- 2,40 -piperidine] based histone deacetylase inhibitors
    European Journal of Medicinal Chemistry 64 (2013) 273-284