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

doi:10.5012/bkcs.2011.32.5.1650

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

Research output: Contribution to journal › Article › peer-review

3 Citations (Scopus)

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 language	English
Pages (from-to)	1650-1656
Number of pages	7
Journal	Bulletin of the Korean Chemical Society
Volume	32
Issue number	5
DOIs	https://doi.org/10.5012/bkcs.2011.32.5.1650
Publication status	Published - 2011 May 20

All Science Journal Classification (ASJC) codes

Chemistry(all)

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10.5012/bkcs.2011.32.5.1650

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title = "Synthesis and evaluation of tricyclic derivatives containing a non-aromatic amide as poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors",

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.",

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AU - Park, Chun Ho

AU - Chun, Kwangwoo

AU - Choi, Jong Hee

AU - Ji, Wan Keun

AU - Kim, Hyun Young

AU - Kim, Seung Hyun

AU - Han, Gyoonhee

AU - Kim, Myung Hwa

PY - 2011/5/20

Y1 - 2011/5/20

N2 - 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.

AB - 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.

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Synthesis and evaluation of tricyclic derivatives containing a non-aromatic amide as poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors

Abstract

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