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

Article Details

Citation

Kim MH, Lee J, Jung K, Kim M, Park YJ, Ahn H, Kwon YH, Hah JM

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

Bioorg Med Chem. 2013 Apr 15;21(8):2271-2285. doi: 10.1016/j.bmc.2013.02.021. Epub 2013 Feb 21.

PubMed ID
23498914 [ View in PubMed
]
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 Kd using SPR, JNK3 kinase assay, and cell-viability of human neuroblastoma cells. Most tested compounds showed high affinity (10 muM-46 nM) to JNK3. Among them, compound 16f exhibited potent activities (Kd=46 nM). Especially, 16f was also found to present a potent cell protective effect (IC50=1.09 muM) against toxicity induced by anisomycin, showing a possibility as protective therapeutics in neuronal cell apoptosis.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
PyrazolanthroneMitogen-activated protein kinase 10IC 50 (nM)10000N/AN/ADetails