Resistance-Modifying agents. 5. 1 Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly (ADP-ribose) polymerase (PARP)

RJ Griffin, S Srinivasan, K Bowman…

Index: Griffin, Roger J.; Srinivasan, Sheila; Bowman, Karen Journal of Medicinal Chemistry, 1998 , vol. 41, # 26 p. 5247 - 5256

Full Text: HTML

Citation Number: 128

Abstract

Clinical studies concerning the role of poly (ADP-ribose) polymerase (PARP) in the repair of drug-and radiation-induced DNA damage have been impeded by the poor solubility, lack of potency, and limited specificity of currently available inhibitors. A series of 2-alkyl-and 2-aryl- substituted 8-hydroxy-, 8-methoxy-, and 8-methylquinazolin-4 (3 H)-ones has been synthesized and evaluated for PARP inhibitory activity in permeabilized L1210 murine ...