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Syntheses and biological evaluation of 1-heteroaryl-2-aryl-1H-benzimidazole derivatives as c-Jun N-terminal kinase inhibitors with neuroprotective effects
- Authors
- Kim, Mi-hyun; Lee, Junghun; Jung, Kyungjin; Kim, Minjung; Park, Yun-Jin; Ahn, Heechul; Kwon, Young Hye; Hah, Jung-Mi
- Issue Date
- Apr-2013
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Benzimidazole; Neuroprotective effect; Neurodegenerative disease; Neuroblastoma cell line; Kinase inhibitor; JNK
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY, v.21, no.8, pp.2271 - 2285
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY
- Volume
- 21
- Number
- 8
- Start Page
- 2271
- End Page
- 2285
- ISSN
- 0968-0896
- Abstract
- 1-Heteroaryl-2-aryl-1H-benzimidazole derivatives were synthesized as inhibitors of c-Jun N-terminal kinases, JNK3. Their activities were evaluated through measurement of K-d using SPR, JNK3 kinase assay, and cell-viability of human neuroblastoma cells. Most tested compounds showed high affinity (10 mu M-46 nM) to JNK3. Among them, compound 16f exhibited potent activities (K-d = 46 nM). Especially, 16f was also found to present a potent cell protective effect (IC50 = 1.09 mu M) against toxicity induced by anisomycin, showing a possibility as protective therapeutics in neuronal cell apoptosis. (C) 2013 Elsevier Ltd. All rights reserved.
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Related Researcher
- Hah, Jung Mi
- COLLEGE OF PHARMACY (DEPARTMENT OF PHARMACY)