Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 하정미 | - |
dc.date.accessioned | 2020-01-22T07:28:03Z | - |
dc.date.available | 2020-01-22T07:28:03Z | - |
dc.date.issued | 2019-12 | - |
dc.identifier.citation | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, v. 35, No. 1, Page. 372-376 | en_US |
dc.identifier.issn | 1475-6366 | - |
dc.identifier.issn | 1475-6374 | - |
dc.identifier.uri | https://www.tandfonline.com/doi/full/10.1080/14756366.2019.1705294 | - |
dc.identifier.uri | https://repository.hanyang.ac.kr/handle/20.500.11754/122222 | - |
dc.description.abstract | 3-alkyl-5-aryl-1-pyrimidyl-1H-pyrazole derivatives were designed and synthesised as selective inhibitors of JNK3, a target for the treatment of neurodegenerative diseases. Following previous studies, we have designed JNK3 inhibitors to reduce the molecular weight and successfully identified a lead compound that exhibits equipotent activity towards JNK3. Kinase profiling results also showed high selectivity for JNK3 among 38 kinases. Among the derivatives, the IC50 value of 8a, (R)-2-(1-(2-((1-(cyclopropanecarbonyl)pyrrolidin-3-yl)amino)pyrimidin-4-yl)-5-(3,4-dichlorophenyl)-1H-pyrazol-3-yl)acetonitrile exhibited 227 nM, showing the highest inhibitory activity against JNK3. | en_US |
dc.description.sponsorship | This work was financially supported by a National Research Foundation of Korea grant [NRF-2017R1A2B4006447 and NRF-2019M3A9A8066500; J.-M. Hah]. | en_US |
dc.language.iso | en_US | en_US |
dc.publisher | TAYLOR & FRANCIS LTD | en_US |
dc.subject | JNK | en_US |
dc.subject | pyrazole | en_US |
dc.subject | neurodegenerative diseases | en_US |
dc.subject | SAR | en_US |
dc.title | Discovery of 3-alkyl-5-aryl-1-pyrimidyl-1H-pyrazole derivatives as a novel selective inhibitor scaffold of JNK3 | en_US |
dc.type | Article | en_US |
dc.relation.no | 1 | - |
dc.relation.volume | 35 | - |
dc.identifier.doi | 10.1080/14756366.2019.1705294 | - |
dc.relation.page | 372-376 | - |
dc.relation.journal | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | - |
dc.contributor.googleauthor | Oh, Y. | - |
dc.contributor.googleauthor | Jang, M. | - |
dc.contributor.googleauthor | Cho, H. | - |
dc.contributor.googleauthor | Yang, S. | - |
dc.contributor.googleauthor | Im, D. | - |
dc.contributor.googleauthor | Moon, H. | - |
dc.contributor.googleauthor | Hah, J.-M. | - |
dc.relation.code | 2019001404 | - |
dc.sector.campus | E | - |
dc.sector.daehak | COLLEGE OF PHARMACY[E] | - |
dc.sector.department | DEPARTMENT OF PHARMACY | - |
dc.identifier.pid | jhah | - |
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