Syntheses and biological evaluation of 1-heteroaryl-2-aryl-1H-benzimidazole derivatives as c-Jun N-terminal kinase inhibitors with neuroprotective effects

M Kim, J Lee, K Jung, M Kim, YJ Park, H Ahn…

文献索引：Kim, Mi-Hyun; Lee, Junghun; Jung, Kyungjin; Kim, Minjung; Park, Yun-Jin; Ahn, Heechul; Kwon, Young Hye; Hah, Jung-Mi Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 8 p. 2271 - 2285

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被引用次数: 8

摘要

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 Kd using SPR, JNK3 kinase assay, and cell-viability of human neuroblastoma cells. Most tested compounds showed high affinity (10μM–46nM) to JNK3. Among them, compound 16f exhibited potent activities (Kd= 46nM). Especially, 16f was also found to present a potent ...