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Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors.
Thaler F, Colombo A, Mai A, Amici R, Bigogno C, Boggio R, Cappa A, Carrara S, Cataudella T, Fusar F, Gianti E, di Ventimiglia SJ, Moroni M, Munari D, Pain G, Regalia N, Sartori L, Vultaggio S, Dondio G, Gagliardi S, Minucci S, Mercurio C, Varasi M. Thaler F, et al. J Med Chem. 2010 Jan 28;53(2):822-39. doi: 10.1021/jm901502p. J Med Chem. 2010. PMID: 20017493
Discovery, synthesis, and pharmacological evaluation of spiropiperidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors.
Varasi M, Thaler F, Abate A, Bigogno C, Boggio R, Carenzi G, Cataudella T, Dal Zuffo R, Fulco MC, Rozio MG, Mai A, Dondio G, Minucci S, Mercurio C. Varasi M, et al. Among authors: thaler f. J Med Chem. 2011 Apr 28;54(8):3051-64. doi: 10.1021/jm200146u. Epub 2011 Apr 1. J Med Chem. 2011. PMID: 21417419
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: thaler f. J Med Chem. 2014 Jun 26;57(12):5333-47. doi: 10.1021/jm500547c. Epub 2014 Jun 11. J Med Chem. 2014. PMID: 24918261
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: thaler f. 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: thaler f. 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: thaler f. 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
85 results