Synthesis and Evaluation of Tricyclic Derivatives Containing a Non-Aromatic Amide as Poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors

Graduate Program in Biomaterials Science and Engineering, Yonsei University, Seoul 120-740, KoreaReceived February 24, 2011, Accepted March 31, 2011A series of potent tricyclic derivatives with a non-aromatic amide as potent PARP-1 inhibitors weresuccessfully synthesized and their PARP-1 inhibitory activity was evaluated. Among the derivatives, 2-(1-propylpiperidin-4-yloxy)-7,8,9,10-tetrahydrophenanthridin-6(5 H)-one 23c displayed potent activity in aPARP-1 enzymatic assay and cell-based assay (IC