Design, synthesis, and biological evaluation of a series of benzo [de][1, 7] naphthyridin-7 (8 H)-ones bearing a functionalized longer chain appendage as novel …

…, XJ Huan, SS Song, Q Liu, Y Chen, J Ding…

Index: Ye, Na; Chen, Chuan-Huizi; Chen, Tiantian; Song, Zilan; He, Jin-Xue; Huan, Xia-Juan; Song, Shan-Shan; Liu, Qiufeng; Chen, Yi; Ding, Jian; Xu, Yechun; Miao, Ze-Hong; Zhang, Ao Journal of Medicinal Chemistry, 2013 , vol. 56, # 7 p. 2885 - 2903

Full Text: HTML

Citation Number: 30

Abstract

A series of benzo [de][1, 7] naphthyridin-7 (8 H)-ones possessing a functionalized long- chain appendage have been designed and evaluated as novel PARP1 inhibitors. The initial effort led to the first-generation PARP1 inhibitor 26 bearing a terminal phthalazin-1 (2 H)-one framework and showing remarkably high PARP1 inhibitory activity (0.31 nM) but only moderate potency in the cell. Further effort generated the second-generation lead 41, ...