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Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models.
Menna M, Fiorentino F, Marrocco B, Lucidi A, Tomassi S, Cilli D, Romanenghi M, Cassandri M, Pomella S, Pezzella M, Del Bufalo D, Zeya Ansari MS, Tomašević N, Mladenović M, Viviano M, Sbardella G, Rota R, Trisciuoglio D, Minucci S, Mattevi A, Rotili D, Mai A. Menna M, et al. Among authors: marrocco b. Eur J Med Chem. 2022 Jul 5;237:114410. doi: 10.1016/j.ejmech.2022.114410. Epub 2022 Apr 27. Eur J Med Chem. 2022. PMID: 35525212
Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.
Rotili D, Tomassi S, Conte M, Benedetti R, Tortorici M, Ciossani G, Valente S, Marrocco B, Labella D, Novellino E, Mattevi A, Altucci L, Tumber A, Yapp C, King ON, Hopkinson RJ, Kawamura A, Schofield CJ, Mai A. Rotili D, et al. Among authors: marrocco b. J Med Chem. 2014 Jan 9;57(1):42-55. doi: 10.1021/jm4012802. Epub 2013 Dec 19. J Med Chem. 2014. PMID: 24325601
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: marrocco b. 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: marrocco b. 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
Polymyxins and quinazolines are LSD1/KDM1A inhibitors with unusual structural features.
Speranzini V, Rotili D, Ciossani G, Pilotto S, Marrocco B, Forgione M, Lucidi A, Forneris F, Mehdipour P, Velankar S, Mai A, Mattevi A. Speranzini V, et al. Among authors: marrocco b. Sci Adv. 2016 Sep 9;2(9):e1601017. doi: 10.1126/sciadv.1601017. eCollection 2016 Sep. Sci Adv. 2016. PMID: 27626075 Free PMC article.
Development of alkyl glycerone phosphate synthase inhibitors: Structure-activity relationship and effects on ether lipids and epithelial-mesenchymal transition in cancer cells.
Stazi G, Battistelli C, Piano V, Mazzone R, Marrocco B, Marchese S, Louie SM, Zwergel C, Antonini L, Patsilinakos A, Ragno R, Viviano M, Sbardella G, Ciogli A, Fabrizi G, Cirilli R, Strippoli R, Marchetti A, Tripodi M, Nomura DK, Mattevi A, Mai A, Valente S. Stazi G, et al. Among authors: marrocco b. Eur J Med Chem. 2019 Feb 1;163:722-735. doi: 10.1016/j.ejmech.2018.11.050. Epub 2018 Nov 28. Eur J Med Chem. 2019. PMID: 30576903
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
Rotili D, Tarantino D, Nawrozkij MB, Babushkin AS, Botta G, Marrocco B, Cirilli R, Menta S, Badia R, Crespan E, Ballante F, Ragno R, Esté JA, Maga G, Mai A. Rotili D, et al. Among authors: marrocco b. J Med Chem. 2014 Jun 26;57(12):5212-25. doi: 10.1021/jm500284x. Epub 2014 Jun 16. J Med Chem. 2014. PMID: 24933420
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: marrocco b. 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.
18 results