Pellicciari, Roberto published the artcileOn the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives, Safety of 4-Hydroxy-2,3-dihydroisoindol-1-one, the main research area is excitotoxins cell death PARP2 inhibitor isoquinoline derivative SAR preparation.
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 pathophysiol. 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 pharmacol. evaluation of a large series of isoquinolinone derivatives as PARP-1/PARP-2 inhibitors. Among them, we identified the 5-benzoyloxyisoquinolin-1(2H)-one derivative as the most selective PARP-2 inhibitor reported so far, with a PARP-2/PARP-1 selectivity index greater than 60.
ChemMedChem published new progress about Cell death. 366453-21-6 belongs to class indole-building-block, name is 4-Hydroxy-2,3-dihydroisoindol-1-one, and the molecular formula is C8H7NO2, Safety of 4-Hydroxy-2,3-dihydroisoindol-1-one.
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles