Development of novel 5-LOX inhibitors with higher activities is highly demanded.  In previous study, we have built a model for the active conformation of human 5-LOX, and identified naphthalen-1-yl 3,5-dinitrobenzoate (JMC-4) as a 5-LOX inhibitor by virtual screening.  Several of them were found with significantly increased activities according to cell-free assay and human whole blood assay.  The structure-activity relationship study may provide useful insights for designing effective 5-LOX inhibitors.
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