Discovery of 3-alkyl-5-aryl-1-pyrimidyl-1H-pyrazole derivatives as a novel selective inhibitor scaffold of JNK3
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 c...
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| Main Authors: | , , , , , , |
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| Format: | Book |
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Taylor & Francis Group,
2020-01-01T00:00:00Z.
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| 001 | doaj_8cf4d412b5ed44ec9b5cedf3e9def8dd | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Youri Oh |e author |
| 700 | 1 | 0 | |a Miyoung Jang |e author |
| 700 | 1 | 0 | |a Hyunwook Cho |e author |
| 700 | 1 | 0 | |a Songyi Yang |e author |
| 700 | 1 | 0 | |a Daseul Im |e author |
| 700 | 1 | 0 | |a Hyungwoo Moon |e author |
| 700 | 1 | 0 | |a Jung-Mi Hah |e author |
| 245 | 0 | 0 | |a Discovery of 3-alkyl-5-aryl-1-pyrimidyl-1H-pyrazole derivatives as a novel selective inhibitor scaffold of JNK3 |
| 260 | |b Taylor & Francis Group, |c 2020-01-01T00:00:00Z. | ||
| 500 | |a 1475-6366 | ||
| 500 | |a 1475-6374 | ||
| 500 | |a 10.1080/14756366.2019.1705294 | ||
| 520 | |a 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. | ||
| 546 | |a EN | ||
| 690 | |a jnk | ||
| 690 | |a pyrazole | ||
| 690 | |a neurodegenerative diseases | ||
| 690 | |a sar | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 35, Iss 1, Pp 372-376 (2020) | |
| 787 | 0 | |n http://dx.doi.org/10.1080/14756366.2019.1705294 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6366 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6374 | |
| 856 | 4 | 1 | |u https://doaj.org/article/8cf4d412b5ed44ec9b5cedf3e9def8dd |z Connect to this object online. |