Table 1.
12-LOX Inhibition of Analogues 1, 8–34a
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compd | R | IC50 [± SD] (µM) |
1 | 2-OH, 3-OMe-Ph | 5.1 [0.5] |
8 | Ph | >40 |
9 | 2-OH-Ph | >40 |
10 | 3-OMe-Ph | >40 |
11 | 2-OMe-Ph | >40 |
12 | 2,3-OMe-Ph | >40 |
13 | 2-NH2-Ph | >40 |
14 | 3-OH-Ph | >40 |
15 | 2-NH2, 3-OMe-Ph | >40 |
16 | 3-OH, 4-OMe-Ph | >40 |
17 | 7-indole | >40 |
18 | 2,3-CI-Ph | >40 |
19 | 3-CI | 6.2 [2.0] |
20 | 3-F | 19 [4] |
21 | 3-Br | 13 [1] |
22 | 4-Br | 2.2 [0.5] |
23 | 3-Me | >40 |
24 | 3-NH2 | >40 |
25 | 3-NO2 | >40 |
26 | 3-allyl | >40 |
27 | 4-Cl | 6.3 [1.0] |
28 | 4-OMe | 22 [11] |
29 | 5-CI | >40 |
30 | 5-OMe | >40 |
31 | 5-NH2 | >40 |
32 | 5-F | >40 |
33 | 5-NO2 | >40 |
34 | 6-OMe | >40 |
IC50 values represent the half maximal (50%) inhibitory concentration as determined in the UV–vis cuvette-based assay in triplicate.