Abstractí¬A series of novel indole derivatives was designed, synthesized and evaluated by cell-based assays for their inhibitory activities
against 5-LOX in rat peritoneal leukocytes. Most of them (30 out of 35) showed an inhibitory potency higher than the initial
screening hit 1a (IC50 = 74 lM). Selected compounds for concentrationĘCresponse studies showed prominent inhibitory activities
with IC50 values ranging from 0.74 lMto 3.17 lM. Four compounds (1m, 1s, 4a, and 6a) exhibited the most potent inhibitory activity
compared to that of the reference drug (Zileuton), with IC50 values less than 1 lM. Molecular modeling studies for compounds
1a, 3a, 4a, and 6a were also presented. The excellent in vitro activities of this class of compounds may possess potential for the treatment
of LT-related diseases.