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Identification and SAR of novel pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).

By Pescatore, Giovanna; Branca, Danila; Fiore, Fabrizio; Kinzel, Olaf; Bufi, Laura Llauger; Muraglia, Ester; Orvieto, Federica; Rowley, Michael; Toniatti, Carlo; Torrisi, Caterina; et al From Bioorganic & Medicinal Chemistry Letters (2010), 20(3), 1094-1099. Language: English, Database: CAPLUS, DOI:10.1016/j.bmcl.2009.12.026 The discovery…

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.

By Ferrigno, Federica; Branca, Danila; Kinzel, Olaf; Lillini, Samuele; Llauger Bufi, Laura; Monteagudo, Edith; Muraglia, Ester; Rowley, Michael; Schultz-Fademrecht, Carsten; Toniatti, Carlo; et al From Bioorganic & Medicinal Chemistry Letters (2010), 20(3), 1100-1105. Language: English, Database: CAPLUS, DOI:10.1016/j.bmcl.2009.11.087 We describe…

Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).

By Torrisi, Caterina; Bisbocci, Monica; Ingenito, Raffaele; Ontoria, Jesus M.; Rowley, Michael; Schultz-Fademrecht, Carsten; Toniatti, Carlo; Jones, Philip From Bioorganic & Medicinal Chemistry Letters (2010), 20(2), 448-452. Language: English, Database: CAPLUS, DOI:10.1016/j.bmcl.2009.12.002 A novel hexahydrobenzonaphthyridinone PARP-1 pharmacophore is reported. Subsequent…

Synthesis and biological evaluation of substituted 2-phenyl-2H-indazole-7-carboxamides as potent poly(ADP-ribose) polymerase (PARP) inhibitors.

By Scarpelli, Rita; Boueres, Julia K.; Cerretani, Mauro; Ferrigno, Federica; Ontoria, Jesus M.; Rowley, Michael; Schultz-Fademrecht, Carsten; Toniatti, Carlo; Jones, Philip From Bioorganic & Medicinal Chemistry Letters (2010), 20(2), 488-492. Language: English, Database: CAPLUS, DOI:10.1016/j.bmcl.2009.11.127 A potent series of substituted…

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