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Page 1
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: botrugno oa. 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
Pure enantiomers of benzoylamino-tranylcypromine: LSD1 inhibition, gene modulation in human leukemia cells and effects on clonogenic potential of murine promyelocytic blasts.
Valente S, Rodriguez V, Mercurio C, Vianello P, Saponara B, Cirilli R, Ciossani G, Labella D, Marrocco B, Monaldi D, Ruoppolo G, Tilset M, Botrugno OA, Dessanti P, Minucci S, Mattevi A, Varasi M, Mai A. Valente S, et al. Among authors: botrugno oa. Eur J Med Chem. 2015 Apr 13;94:163-74. doi: 10.1016/j.ejmech.2015.02.060. Epub 2015 Mar 3. Eur J Med Chem. 2015. PMID: 25768700
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: botrugno oa. 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
Tranylcypromine-Based LSD1 Inhibitors: Structure-Activity Relationships, Antiproliferative Effects in Leukemia, and Gene Target Modulation.
Fioravanti R, Romanelli A, Mautone N, Di Bello E, Rovere A, Corinti D, Zwergel C, Valente S, Rotili D, Botrugno OA, Dessanti P, Vultaggio S, Vianello P, Cappa A, Binda C, Mattevi A, Minucci S, Mercurio C, Varasi M, Mai A. Fioravanti R, et al. Among authors: botrugno oa. ChemMedChem. 2020 Apr 3;15(7):643-658. doi: 10.1002/cmdc.201900730. Epub 2020 Feb 14. ChemMedChem. 2020. PMID: 32003940 Free PMC article.
Pure Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies.
Valente S, Rodriguez V, Mercurio C, Vianello P, Saponara B, Cirilli R, Ciossani G, Labella D, Marrocco B, Ruoppolo G, Botrugno OA, Dessanti P, Minucci S, Mattevi A, Varasi M, Mai A. Valente S, et al. Among authors: botrugno oa. ACS Med Chem Lett. 2014 Dec 8;6(2):173-7. doi: 10.1021/ml500424z. eCollection 2015 Feb 12. ACS Med Chem Lett. 2014. PMID: 25699146 Free PMC article.
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: botrugno oa. 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
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: botrugno oa. 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
33 results