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. Author manuscript; available in PMC: 2014 Mar 27.
Published in final edited form as: J Med Chem. 2014 Jan 6;57(2):495–506. doi: 10.1021/jm4016476

Table 1.

12-LOX Inhibition of Analogues 1, 8–34a

graphic file with name nihms561588t1.jpg
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
a

IC50 values represent the half maximal (50%) inhibitory concentration as determined in the UV–vis cuvette-based assay in triplicate.