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Discovery of 3-alkyl-5-aryl-1-pyrimidyl-1H-pyrazole derivatives as a novel selective inhibitor scaffold of JNK3open access
- Authors
- Oh, Youri; Jang, Miyoung; Cho, Hyunwook; Yang, Songyi; Im, Daseul; Moon, Hyungwoo; Hah, Jung-Mi
- Issue Date
- Jan-2020
- Publisher
- Taylor and Francis Ltd
- Keywords
- JNK; neurodegenerative diseases; pyrazole; SAR
- Citation
- Journal of Enzyme Inhibition and Medicinal Chemistry, v.35, no.1, pp 372 - 376
- Pages
- 5
- Indexed
- SCIE
SCOPUS
- Journal Title
- Journal of Enzyme Inhibition and Medicinal Chemistry
- Volume
- 35
- Number
- 1
- Start Page
- 372
- End Page
- 376
- ISSN
- 1475-6366
1475-6374
- 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. © 2019, © 2019 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.
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Related Researcher
- Hah, Jung Mi
- COLLEGE OF PHARMACY (DEPARTMENT OF PHARMACY)