Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly (ADP-ribose) polymerase-1 inhibitors

…, MC Palumbi, M Rowley, C Toniatti, E Muraglia

文献索引：Branca, Danila; Cerretani, Mauro; Jones, Philip; Koch, Uwe; Orvieto, Federica; Palumbi, Maria Cecilia; Rowley, Michael; Toniatti, Carlo; Muraglia, Ester Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 15 p. 4042 - 4045

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被引用次数: 16

摘要

PARP inhibitors have been demonstrated to retard intracellular DNA repair and therefore sensitize tumor cells to cytotoxic agents or ionizing radiation. We report the identification of a novel class of PARP1 inhibitors, containing a pyrrolo moiety fused to a dihydroisoquinolinone, derived from virtual screening of the proprietary collection. SAR exploration around the nitrogen of the aminoethyl appendage chain of 1 led to ...