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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 3.

12-LOX Inhibition of Analogues 69–83a

graphic file with name nihms561588t3.jpg

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
a

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

b

Represents percent inhibition at 25 µM.

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