Discovery of 1-substituted benzyl-quinazoline-2,4(1H,3H)-dione derivatives as novel poly(ADP-ribose)polymerase-1 inhibitors

A series of novel quinazoline-2,4(1H,3H)-dione derivatives were synthesized and evaluated as inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). X, Y = H or F; R1 = a range of amino acid fragments; IC50: 9.51-5290 nM.