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ID: ALA1153049

Journal: Bioorg Med Chem Lett

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

Authors: Branca D, Cerretani M, Jones P, Koch U, Orvieto F, Palumbi MC, Rowley M, Toniatti C, Muraglia E.

Abstract: 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 compounds that displayed low nanomolar activity in a PARP1 enzymatic assay.

CiteXplore: 19553107

DOI: 10.1016/j.bmcl.2009.06.031