Design and synthesis of poly ADP-ribose polymerase-1 inhibitors. 2. Biological evaluation of aza-5 [H]-phenanthridin-6-ones as potent, aqueous-soluble compounds …

…, L Serdyuk, C Alemu, C Bradford, T Chiou…

Index: Ferraris, Dana; Ko, Yao-Sen; Pahutski, Thomas; Ficco, Rica Pargas; Serdyuk, Larisa; Alemu, Christina; Bradford, Chadwick; Chiou, Tiffany; Hoover, Randall; Huang, Shirley; Lautar, Susan; Liang, Shi; Lin, Qian; Lu, May X.-C.; Mooney, Maria; Morgan, Lisa; Qian, Yongzhen; Tran, Scott; Williams, Lawrence R.; Wu, Qi Yi; Zhang, Jie; Zou, Yinong; Kalish, Vincent Journal of Medicinal Chemistry, 2003 , vol. 46, # 14 p. 3138 - 3151

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Citation Number: 73

Abstract

A series of aza-5 [H]-phenanthridin-6-ones were synthesized and evaluated as inhibitors of poly ADP-ribose polymerase-1 (PARP-1). Inhibitory potency of the unsubstituted aza-5 [H]- phenanthridin-6-ones (ie, benzonaphthyridones) was dependent on the position of the nitrogen atom within the core structure. The A ring nitrogen analogues (7-, 8-, and 10-aza-5 [H]-phenanthridin-6-ones) were an order of magnitude less potent than C ring nitrogen ...