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

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Abstract

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.

Original languageEnglish
Pages (from-to)1650-1656
Number of pages7
JournalBulletin of the Korean Chemical Society
Volume32
Issue number5
DOIs
Publication statusPublished - 2011 May 20

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All Science Journal Classification (ASJC) codes

  • Chemistry(all)

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