Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 김승현 | - |
dc.date.accessioned | 2018-03-19T04:21:07Z | - |
dc.date.available | 2018-03-19T04:21:07Z | - |
dc.date.issued | 2012-08 | - |
dc.identifier.citation | Medicinal Chemistry Research, Aug 2012, 21(8), P.1533-1543 | en_US |
dc.identifier.issn | 1554-8120 | - |
dc.identifier.issn | 1054-2523 | - |
dc.identifier.uri | https://link.springer.com/article/10.1007%2Fs00044-011-9673-6 | - |
dc.identifier.uri | http://hdl.handle.net/20.500.11754/48806 | - |
dc.description.abstract | A series of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors, 5-oxo-2,4,5,6-tetrahydro-1H-thiopyrano[3,4-c]quinoline-9-carboxamide derivatives, were successfully synthesized and their PARP-1 inhibitory activity was evaluated. These compounds were prepared from carboxylic acid 7 and the appropriate amines, and a number of the synthesized compounds were found to have significant PARP-1 activity. Among them, 9m showed potent activity in a PARP-1 enzymatic assay and cell-based assay (IC50 = 0.045 μM, ED50 = 0.54 μM). Molecular modeling studies confirmed the obtained biological results. | en_US |
dc.description.sponsorship | This study was supported by a grant from the Korea Healthcare Technology R&D Project, Ministry for Health, Welfare & Family Affairs, Republic of Korea (A100453-1001-0000100). We thank Professor Gyoonhee Han (Department of Biotechnology, Yonsei University, Republic of Korea) for his assistance with the docking study. | en_US |
dc.language.iso | en | en_US |
dc.publisher | Springer Science + Business Media | en_US |
dc.subject | Poly(ADP-ribose)polymerase | en_US |
dc.subject | PARP-1 inhibitor | en_US |
dc.subject | Thiopyranoquinoline derivatives | en_US |
dc.title | Synthesis and evaluation of thiopyrano[3,4-c]quinoline-9-carboxamide derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1) | en_US |
dc.type | Article | en_US |
dc.relation.volume | 21 | - |
dc.identifier.doi | 10.1007/s00044-011-9673-6 | - |
dc.relation.page | 1533-1543 | - |
dc.relation.journal | MEDICINAL CHEMISTRY RESEARCH | - |
dc.contributor.googleauthor | Park, Chun-Ho | - |
dc.contributor.googleauthor | Chun, Kwangwoo | - |
dc.contributor.googleauthor | Joe, Bo-Young | - |
dc.contributor.googleauthor | Choi, Jong-Hee | - |
dc.contributor.googleauthor | Lee, Han-Chang | - |
dc.contributor.googleauthor | Ku, Il-Whea | - |
dc.contributor.googleauthor | Kim, Hyun Young | - |
dc.contributor.googleauthor | Koh, Seong-Ho | - |
dc.contributor.googleauthor | Cho, Goang Won | - |
dc.contributor.googleauthor | Kim, Seung Hyun | - |
dc.relation.code | 2012206601 | - |
dc.sector.campus | S | - |
dc.sector.daehak | COLLEGE OF MEDICINE[S] | - |
dc.sector.department | DEPARTMENT OF MEDICINE | - |
dc.identifier.pid | kimsh1 | - |
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