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Abstract A series of novel 1,2,3-benzotriazin-4-one derivatives were designed, synthesized and their inhibitory activities against leukotriene A 4 hydrolase aminopeptidase in vitro were evaluated. Many compounds showed moderate to good… Click to show full abstract
Abstract A series of novel 1,2,3-benzotriazin-4-one derivatives were designed, synthesized and their inhibitory activities against leukotriene A 4 hydrolase aminopeptidase in vitro were evaluated. Many compounds showed moderate to good activities at the concentration of 10 μmol/L. Among them, compound IV-16 exhibited the highest inhibitory activity up to 80.6% with an IC 50 of 1.30 ± 0.20 μmol/L. The compound IV-16 was also tested the proliferation inhibitory activities in THP1 human AML cell line and its binding model with LTA 4 H enzyme by molecular docking was studied. It indicated that 1,2,3-benzotriazin-4-one was a promising scaffold for further study. The relationship between structure and inhibitory activity was also preliminarily discussed.
Journal Title: Chinese Chemical Letters
Year Published: 2017
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