Synthesis and study of new 4-quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP)

Abstract

4-Quinazolinones modified with 2,2,5,5-tetramethyl-2,5-dihydro-1H-pyrrole or 2,2,6,6tetramethyl-1,2,3,6-tetrahydropyridine rings and their N-oxyl derivatives were synthesized and some of them evaluated for protecting activity against H 2 O 2 induced cell death on WRL-68 human liver cell line. Compounds 15a, 15c and 15d exhibited remarkably inhibitory effects on PARP enzyme in vitro.