Synthesis and evaluation of thiopyrano[3,4-c]quinoline-9-carboxamide derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1)
DC Field | Value | Language |
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dc.contributor.author | Park, Chun-Ho | - |
dc.contributor.author | Chun, Kwangwoo | - |
dc.contributor.author | Joe, Bo-Young | - |
dc.contributor.author | Choi, Jong-Hee | - |
dc.contributor.author | Lee, Han-Chang | - |
dc.contributor.author | Ku, Il-Whea | - |
dc.contributor.author | Kim, Hyun Young | - |
dc.contributor.author | Koh, Seong-Ho | - |
dc.contributor.author | Cho, Goang Won | - |
dc.contributor.author | Kim, Seung Hyun | - |
dc.contributor.author | Kim, Myung-Hwa | - |
dc.date.accessioned | 2022-07-16T14:22:15Z | - |
dc.date.available | 2022-07-16T14:22:15Z | - |
dc.date.created | 2021-05-12 | - |
dc.date.issued | 2012-08 | - |
dc.identifier.issn | 1054-2523 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/hanyang/handle/2021.sw.hanyang/164972 | - |
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 mu M, ED50 = 0.54 mu M). Molecular modeling studies confirmed the obtained biological results. | - |
dc.language | 영어 | - |
dc.language.iso | en | - |
dc.publisher | SPRINGER | - |
dc.title | Synthesis and evaluation of thiopyrano[3,4-c]quinoline-9-carboxamide derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1) | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Kim, Hyun Young | - |
dc.contributor.affiliatedAuthor | Koh, Seong-Ho | - |
dc.contributor.affiliatedAuthor | Kim, Seung Hyun | - |
dc.identifier.doi | 10.1007/s00044-011-9673-6 | - |
dc.identifier.scopusid | 2-s2.0-84866109824 | - |
dc.identifier.wosid | 000305559900001 | - |
dc.identifier.bibliographicCitation | MEDICINAL CHEMISTRY RESEARCH, v.21, no.8, pp.1533 - 1543 | - |
dc.relation.isPartOf | MEDICINAL CHEMISTRY RESEARCH | - |
dc.citation.title | MEDICINAL CHEMISTRY RESEARCH | - |
dc.citation.volume | 21 | - |
dc.citation.number | 8 | - |
dc.citation.startPage | 1533 | - |
dc.citation.endPage | 1543 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.isOpenAccess | N | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.subject.keywordPlus | CELL-DEATH | - |
dc.subject.keywordPlus | DNA-DAMAGE | - |
dc.subject.keywordPlus | CHEMOPOTENTIATION | - |
dc.subject.keywordPlus | TEMOZOLOMIDE | - |
dc.subject.keywordPlus | DISCOVERY | - |
dc.subject.keywordPlus | DEPLETION | - |
dc.subject.keywordPlus | NAD(+) | - |
dc.subject.keywordPlus | CANCER | - |
dc.subject.keywordPlus | POTENT | - |
dc.subject.keywordPlus | SITE | - |
dc.subject.keywordAuthor | Poly(ADP-ribose)polymerase | - |
dc.subject.keywordAuthor | PARP-1 inhibitor | - |
dc.subject.keywordAuthor | Thiopyranoquinoline derivatives | - |
dc.identifier.url | https://link.springer.com/article/10.1007/s00044-011-9673-6 | - |
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