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83. 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 (2017) Thieno[3,2-b]pyrrole-5-carboxamides as new reversible inhibitors
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84. Speranzini V, Rotili D, Ciossani G, Pilotto S, Marrocco B, Forgione M, Lucidi A, Forneris F,
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KDM1A inhibitors with unusual structural features. Sci Adv 2:e1601017
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compounds (PAINS) from screening libraries and for their exclusion in bioassays. J Med Chem
53:2719–2740
78. Fiskus W, Sharma S, Shah B, Portier BP, Devaraj SG, Liu K, Iyer SP, Bearss D, Bhalla KN
(2014) Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone
deacetylase inhibitor against human AML cells. Leukemia 28:2155–2164
79. Mould DP, Alli C, Bremberg U, Cartic S, Jordan AM, Geitmann M, Maiques-Diaz A,
McGonagle AE, Somervaille TCP, Spencer GJ, Turlais F, Ogilvie DJ (2017) Development of
(4-cyanophenyl)glycine derivatives as reversible inhibitors of lysine specific demethylase
1. J Med Chem 60:7984–7999
80. Mould DP, Bremberg U, Jordan AM, Geitmann M, Maiques-Diaz A, McGonagle AE, Small
HF, Somervaille TCP, Ogilvie DJ (2017) Development of 5-hydroxypyrazole derivatives as
reversible inhibitors of lysine specific demethylase 1. Bioorg Med Chem Lett 27:3190–3195
81. Mould DP, Bremberg U, Jordan AM, Geitmann M, McGonagle AE, Somervaille TCP, Spencer
GJ, Ogilvie DJ (2017) Development and evaluation of 4-(pyrrolidin-3-yl)benzonitrile derivatives as inhibitors of lysine specific demethylase 1. Bioorg Med Chem Lett 27:4755–4759
82. 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
(2017) 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. J Med Chem 60:1693–1715
83. 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 (2017) 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 60:1673–1692
84. Speranzini V, Rotili D, Ciossani G, Pilotto S, Marrocco B, Forgione M, Lucidi A, Forneris F,
Mehdipour P, Velankar S, Mai A, Mattevi A (2016) Polymyxins and quinazolines are LSD1/
KDM1A inhibitors with unusual structural features. Sci Adv 2:e1601017
Lysine-Specific Histone Demethylases 1/2 (LSD1/2) and Their Inhibitors
219