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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 32, Number 5
BKCSDE 32(5)
May 20, 2011 

Synthesis and Evaluation of Tricyclic Derivatives Containing a Non-Aromatic Amide as Poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors
Chun-Ho Park, Kwangwoo Chun, Jong-Hee Choi, Wan-Keun Ji, Hyun Young Kim, Seung Hyun Kim, Gyoonhee Han, Myung-Hwa Kim*,
Poly(ADP-ribose)polymerase, PARP-1 inhibitor, Phenanthridines
A series of potent tricyclic derivatives with a non-aromatic amide as potent PARP-1 inhibitors were successfully synthesized and their PARP-1 inhibitory activity was evaluated. Among the derivatives, 2-(1- propylpiperidin-4-yloxy)-7,8,9,10-tetrahydrophenanthridin-6(5H)-one 23c displayed potent activity in a PARP-1 enzymatic assay and cell-based assay (IC50 = 0.142 μM, ED50 = 0.90 μM) with good water solubility. Further, molecular modeling studies confirmed the obtained biological results.
1650 - 1656
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