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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: toniatti c. J Med Chem. 2009 Nov 26;52(22):7170-85. doi: 10.1021/jm901188v. J Med Chem. 2009. PMID: 19873981
Development of substituted 6-[4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl]-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells.
Ferrigno F, Branca D, Kinzel O, Lillini S, Llauger Bufi L, Monteagudo E, Muraglia E, Rowley M, Schultz-Fademrecht C, Toniatti C, Torrisi C, Jones P. Ferrigno F, et al. Among authors: toniatti c. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1100-5. doi: 10.1016/j.bmcl.2009.11.087. Epub 2009 Nov 22. Bioorg Med Chem Lett. 2010. PMID: 20022747
A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies.
Kinzel O, Fattori D, Muraglia E, Gallinari P, Nardi MC, Paolini C, Roscilli G, Toniatti C, Gonzalez Paz O, Laufer R, Lahm A, Tramontano A, Cortese R, De Francesco R, Ciliberto G, Koch U. Kinzel O, et al. Among authors: toniatti c. J Med Chem. 2006 Sep 7;49(18):5404-7. doi: 10.1021/jm060516e. J Med Chem. 2006. PMID: 16942012
SAR evolution towards potent C-terminal carboxamide peptide inhibitors of Zika virus NS2B-NS3 protease.
Colarusso S, Ferrigno F, Ponzi S, Pavone F, Conte I, Abate L, Beghetto E, Missineo A, Amaudrut J, Bresciani A, Paonessa G, Tomei L, Montalbetti C, Bianchi E, Toniatti C, Ontoria JM. Colarusso S, et al. Among authors: toniatti c. Bioorg Med Chem. 2022 Mar 1;57:116631. doi: 10.1016/j.bmc.2022.116631. Epub 2022 Jan 23. Bioorg Med Chem. 2022. PMID: 35123179
86 results