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Synthesis and evaluation of tricyclic derivatives containing a non-aromatic amide as inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1)
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| DC Field | Value | Language |
|---|---|---|
| dc.contributor.author | Park, Chun-Ho | - |
| dc.contributor.author | Chun, Kwangwoo | - |
| dc.contributor.author | Joe, Bo-Young | - |
| dc.contributor.author | Park, Ji-Seon | - |
| dc.contributor.author | Kim, Young-Chul | - |
| dc.contributor.author | Choi, Ji-Soo | - |
| dc.contributor.author | Ryu, Dong-Kyu | - |
| 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 | 2022-12-20T18:23:40Z | - |
| dc.date.available | 2022-12-20T18:23:40Z | - |
| dc.date.issued | 2010-04 | - |
| dc.identifier.issn | 0960-894X | - |
| dc.identifier.issn | 1464-3405 | - |
| dc.identifier.uri | https://scholarworks.bwise.kr/hanyang/handle/2021.sw.hanyang/175218 | - |
| dc.description.abstract | Highly potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors, including 9-hydroxy-1,2-dihydro-4H-thiopyrano[ 3,4-c]quinolin-5(6H)-one derivatives with a non-aromatic A-ring, were synthesized. Among the derivatives, 12a showed low nanomolar enzyme and cellular activity (IC50 = 42 nM, ED50 = 220 nM) with good water solubility. Further, 12a exhibited microsomal stability in vitro and brain permeability in vivo. | - |
| dc.format.extent | 4 | - |
| dc.language | 영어 | - |
| dc.language.iso | ENG | - |
| dc.publisher | Pergamon Press Ltd. | - |
| dc.title | Synthesis and evaluation of tricyclic derivatives containing a non-aromatic amide as inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1) | - |
| dc.type | Article | - |
| dc.publisher.location | 영국 | - |
| dc.identifier.doi | 10.1016/j.bmcl.2010.02.014 | - |
| dc.identifier.scopusid | 2-s2.0-77949654750 | - |
| dc.identifier.wosid | 000275805900042 | - |
| dc.identifier.bibliographicCitation | Bioorganic & Medicinal Chemistry Letters, v.20, no.7, pp 2250 - 2253 | - |
| dc.citation.title | Bioorganic & Medicinal Chemistry Letters | - |
| dc.citation.volume | 20 | - |
| dc.citation.number | 7 | - |
| dc.citation.startPage | 2250 | - |
| dc.citation.endPage | 2253 | - |
| dc.type.docType | Article | - |
| dc.description.isOpenAccess | N | - |
| dc.description.journalRegisteredClass | sci | - |
| dc.description.journalRegisteredClass | scie | - |
| dc.description.journalRegisteredClass | scopus | - |
| dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
| dc.relation.journalResearchArea | Chemistry | - |
| dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
| dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
| dc.subject.keywordPlus | POLYMERASE-1 INHIBITORS | - |
| dc.subject.keywordPlus | POTENT | - |
| dc.subject.keywordPlus | DISCOVERY | - |
| dc.subject.keywordPlus | DESIGN | - |
| dc.subject.keywordPlus | CANCER | - |
| dc.subject.keywordAuthor | Poly(ADP-ribose)polymerase PARP-1 | - |
| dc.subject.keywordAuthor | Tricyclic derivatives | - |
| dc.identifier.url | https://www.sciencedirect.com/science/article/pii/S0960894X10002040?via%3Dihub | - |
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Related Researcher
- Koh, Seong-Ho
- 서울 의과대학 (DEPARTMENT OF NEUROLOGY)