On the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives.

Abstract

PARP-1 and PARP-2 are members of the family of poly(ADP-ribose)polymerases, which are involved in the maintenance of genomic integrity under conditions of genotoxic stimuli. The different roles of the two isoforms under pathophysiological conditions have not yet been fully clarified, and this is partially due to the lack of selective inhibitors. We report herein the synthesis and preliminary pharmacological evaluation of a large series of isoquinolinone derivatives as PARP-1/PARP-2 inhibitors. Among them, we identified the 5-benzoyloxyisoquinolin-1(2 H)-one derivative as the most selective PARP-2 inhibitor reported so far, with a PARP-2/PARP-1 selectivity index greater than 60.

DOI: 10.1002/cmdc.200800010

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@article{Pellicciari2008OnTW, title={On the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives.}, author={Roberto Pellicciari and Emidio Camaioni and Gabriele Costantino and Laura Formentini and Paola Sabbatini and Francesco Venturoni and G{\"{o}kçen Eren and Daniele Bellocchi and Alberto Chiarugi and Flavio Moroni}, journal={ChemMedChem}, year={2008}, volume={3 6}, pages={914-23} }