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Combined Peptide and Small-Molecule Approach toward Nonacidic THIQ Inhibitors of the KEAP1/NRF2 Interaction.
Ontoria JM, Biancofiore I, Fezzardi P, Ferrigno F, Torrente E, Colarusso S, Bianchi E, Andreini M, Patsilinakos A, Kempf G, Augustin M, Steinbacher S, Summa V, Pacifici R, Muñoz-Sanjuan I, Park L, Bresciani A, Dominguez C, Sherman LT, Harper S. Ontoria JM, et al. Among authors: ferrigno f. ACS Med Chem Lett. 2020 Apr 3;11(5):740-746. doi: 10.1021/acsmedchemlett.9b00594. eCollection 2020 May 14. ACS Med Chem Lett. 2020. PMID: 32435379 Free PMC article.
Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors.
Scarpelli R, Di Marco A, Ferrigno F, Laufer R, Marcucci I, Muraglia E, Ontoria JM, Rowley M, Serafini S, Steinkühler C, Jones P. Scarpelli R, et al. Among authors: ferrigno f. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6078-82. doi: 10.1016/j.bmcl.2008.10.041. Epub 2008 Oct 12. Bioorg Med Chem Lett. 2008. PMID: 18952417
Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.
Jones P, Altamura S, Boueres J, Ferrigno F, Fonsi M, Giomini C, Lamartina S, Monteagudo E, Ontoria JM, Orsale MV, Palumbi MC, Pesci S, Roscilli G, Scarpelli R, Schultz-Fademrecht C, Toniatti C, Rowley M. Jones P, et al. Among authors: ferrigno f. J Med Chem. 2009 Nov 26;52(22):7170-85. doi: 10.1021/jm901188v. J Med Chem. 2009. PMID: 19873981
Identification of novel, selective, and stable inhibitors of class II histone deacetylases. Validation studies of the inhibition of the enzymatic activity of HDAC4 by small molecules as a novel approach for cancer therapy.
Ontoria JM, Altamura S, Di Marco A, Ferrigno F, Laufer R, Muraglia E, Palumbi MC, Rowley M, Scarpelli R, Schultz-Fademrecht C, Serafini S, Steinkühler C, Jones P. Ontoria JM, et al. Among authors: ferrigno f. J Med Chem. 2009 Nov 12;52(21):6782-9. doi: 10.1021/jm900555u. J Med Chem. 2009. PMID: 19888759
Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs.
Ontoria JM, Paonessa G, Ponzi S, Ferrigno F, Nizi E, Biancofiore I, Malancona S, Graziani R, Roberts D, Willis P, Bresciani A, Gennari N, Cecchetti O, Monteagudo E, Orsale MV, Veneziano M, Di Marco A, Cellucci A, Laufer R, Altamura S, Summa V, Harper S. Ontoria JM, et al. Among authors: ferrigno f. ACS Med Chem Lett. 2016 Mar 5;7(5):454-9. doi: 10.1021/acsmedchemlett.5b00468. eCollection 2016 May 12. ACS Med Chem Lett. 2016. PMID: 27190592 Free PMC article.
Improved Selective Class I HDAC and Novel Selective HDAC3 Inhibitors: Beyond Hydroxamic Acids and Benzamides.
Bresciani A, Ontoria JM, Biancofiore I, Cellucci A, Ciammaichella A, Di Marco A, Ferrigno F, Francone A, Malancona S, Monteagudo E, Nizi E, Pace P, Ponzi S, Rossetti I, Veneziano M, Summa V, Harper S. Bresciani A, et al. Among authors: ferrigno f. ACS Med Chem Lett. 2018 Nov 27;10(4):481-486. doi: 10.1021/acsmedchemlett.8b00517. eCollection 2019 Apr 11. ACS Med Chem Lett. 2018. PMID: 30996783 Free PMC article.
Optimization of 2-(1H-imidazo-2-yl)piperazines series of Trypanosoma brucei growth inhibitors as potential treatment for the second stage of HAT.
Ciammaichella A, Ferrigno F, Basta A, D'Amico M, Biancofiore I, Nardi V, Ponzi S, Graziani R, Gennari N, Vittoria Orsale M, Fini I, Paonessa G, Summa V, Harper S, Ontoria JM. Ciammaichella A, et al. Among authors: ferrigno f. Bioorg Med Chem Lett. 2020 Jun 15;30(12):127207. doi: 10.1016/j.bmcl.2020.127207. Epub 2020 Apr 21. Bioorg Med Chem Lett. 2020. PMID: 32354566
31 results