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Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 2: Structure-Based Drug Design and Structure-Activity Relationship.
Vianello P, Sartori L, Amigoni F, Cappa A, Fagá G, Fattori R, Legnaghi E, Ciossani G, Mattevi A, Meroni G, Moretti L, Cecatiello V, Pasqualato S, Romussi A, Thaler F, Trifiró P, Villa M, Botrugno OA, Dessanti P, Minucci S, Vultaggio S, Zagarrí E, Varasi M, Mercurio C. Vianello P, et al. Among authors: villa m. J Med Chem. 2017 Mar 9;60(5):1693-1715. doi: 10.1021/acs.jmedchem.6b01019. Epub 2017 Feb 27. J Med Chem. 2017. PMID: 28186757
Synthesis, biological activity and mechanistic insights of 1-substituted cyclopropylamine derivatives: a novel class of irreversible inhibitors of histone demethylase KDM1A.
Vianello P, Botrugno OA, Cappa A, Ciossani G, Dessanti P, Mai A, Mattevi A, Meroni G, Minucci S, Thaler F, Tortorici M, Trifiró P, Valente S, Villa M, Varasi M, Mercurio C. Vianello P, et al. Among authors: villa m. Eur J Med Chem. 2014 Oct 30;86:352-63. doi: 10.1016/j.ejmech.2014.08.068. Epub 2014 Aug 27. Eur J Med Chem. 2014. PMID: 25173853
Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent.
Vianello P, Botrugno OA, Cappa A, Dal Zuffo R, Dessanti P, Mai A, Marrocco B, Mattevi A, Meroni G, Minucci S, Stazi G, Thaler F, Trifiró P, Valente S, Villa M, Varasi M, Mercurio C. Vianello P, et al. Among authors: villa m. J Med Chem. 2016 Feb 25;59(4):1501-17. doi: 10.1021/acs.jmedchem.5b01209. Epub 2016 Jan 7. J Med Chem. 2016. PMID: 26702542
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.
Sartori L, Mercurio C, Amigoni F, Cappa A, Fagá G, Fattori R, Legnaghi E, Ciossani G, Mattevi A, Meroni G, Moretti L, Cecatiello V, Pasqualato S, Romussi A, Thaler F, Trifiró P, Villa M, Vultaggio S, Botrugno OA, Dessanti P, Minucci S, Zagarrí E, Carettoni D, Iuzzolino L, Varasi M, Vianello P. Sartori L, et al. Among authors: villa m. J Med Chem. 2017 Mar 9;60(5):1673-1692. doi: 10.1021/acs.jmedchem.6b01018. Epub 2017 Feb 27. J Med Chem. 2017. PMID: 28186755
Discovery of Reversible Inhibitors of KDM1A Efficacious in Acute Myeloid Leukemia Models.
Romussi A, Cappa A, Vianello P, Brambillasca S, Cera MR, Dal Zuffo R, Fagà G, Fattori R, Moretti L, Trifirò P, Villa M, Vultaggio S, Cecatiello V, Pasqualato S, Dondio G, So CWE, Minucci S, Sartori L, Varasi M, Mercurio C. Romussi A, et al. Among authors: villa m. ACS Med Chem Lett. 2020 Feb 13;11(5):754-759. doi: 10.1021/acsmedchemlett.9b00604. eCollection 2020 May 14. ACS Med Chem Lett. 2020. PMID: 32435381 Free PMC article.
3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors.
Pevarello P, Fancelli D, Vulpetti A, Amici R, Villa M, Pittalà V, Vianello P, Cameron A, Ciomei M, Mercurio C, Bischoff JR, Roletto F, Varasi M, Brasca MG. Pevarello P, et al. Among authors: villa m. Bioorg Med Chem Lett. 2006 Feb 15;16(4):1084-90. doi: 10.1016/j.bmcl.2005.10.071. Epub 2005 Nov 14. Bioorg Med Chem Lett. 2006. PMID: 16290148
Cinnamic anilides as new mitochondrial permeability transition pore inhibitors endowed with ischemia-reperfusion injury protective effect in vivo.
Fancelli D, Abate A, Amici R, Bernardi P, Ballarini M, Cappa A, Carenzi G, Colombo A, Contursi C, Di Lisa F, Dondio G, Gagliardi S, Milanesi E, Minucci S, Pain G, Pelicci PG, Saccani A, Storto M, Thaler F, Varasi M, Villa M, Plyte S. Fancelli D, et al. Among authors: villa m. J Med Chem. 2014 Jun 26;57(12):5333-47. doi: 10.1021/jm500547c. Epub 2014 Jun 11. J Med Chem. 2014. PMID: 24918261
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.
Pevarello P, Brasca MG, Amici R, Orsini P, Traquandi G, Corti L, Piutti C, Sansonna P, Villa M, Pierce BS, Pulici M, Giordano P, Martina K, Fritzen EL, Nugent RA, Casale E, Cameron A, Ciomei M, Roletto F, Isacchi A, Fogliatto G, Pesenti E, Pastori W, Marsiglio A, Leach KL, Clare PM, Fiorentini F, Varasi M, Vulpetti A, Warpehoski MA. Pevarello P, et al. Among authors: villa m. J Med Chem. 2004 Jun 17;47(13):3367-80. doi: 10.1021/jm031145u. J Med Chem. 2004. PMID: 15189033
1,413 results