Table 3.
12-LOX Inhibition of Analogues 69–83a
![]() | ||||
---|---|---|---|---|
12-LOX |
15-LOX-1 |
|||
compd | R | IC50 [± SD] (µM) |
IC50 [± SD] (µM) |
% inhb |
69 | Ph | 4.5 [0.4] | 49 | |
70 | 1-naphthalene | 1.6 [0.2] | 70 | |
71 | 2-benzothiazole | 1.3 [0.2] | 1.3 [0.2] | |
72 | 2-naphthalene | 2.3 [0.3] | 75 | |
73 | 4-bi-Ph | 4.2 [1.0] | 73 | |
74 | 8-isoquinoline | 4.5 [0.8] | 63 | |
75 | 3-quinoline | 5.3 [0.7] | 58 | |
76 | 4-piperidine-Ph | 6.3 [3.0] | 4 | |
77 | Ph | 2.9 [0.4] | 82 | |
78 | 1-naphthalene | 1.3 [0.3] | 83 | |
79 | 2-benzothiazole | 1.7 [0.8] | 100 | |
80 | 3-quinoline | 2.3 [0.5] | 74 | |
81 | 2-naphthalene | 2.2 [0.3] | 78 | |
82 | 4-bi-Ph | 2.5 [0.4] | 80 | |
83 | 8-quinoline | 5.6 [2.0] | 55 |
IC50 values represent the half maximal (50%) inhibitory concentration as determined in the UV–vis cuvette-based assay in triplicate.
Represents percent inhibition at 25 µM.