Table 2.
Structure of ALS-31 derivatives and their effect on SmSOD activity.
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Code | ID | n | m | R | R1 | Residual SOD Activity (%) in the Presence of [Compound] (a) |
IC50
(µM) (b) |
|
50 µM | 100 µM | |||||||
1098459 | ALS-31-1 | 1 | - | - |
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104.1 | 97.2 | n.d. |
1098464 | ALS-31-2 | 1 | - | - |
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89.8 | 113.1 | n.d. |
1098679 | ALS-31-3 | 1 | 2 | H |
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78.8 | 103.6 | n.d. |
1098687 | ALS-31-4 | - | - | - | - | 92.6 | 96.8 | n.d. |
1098708 | ALS-31-5 | - | - | - | - | 93.4 | 99.6 | n.d. |
1097658 | ALS-31-6 | - | 3 | - | - | 75.1 | 78.0 | 127 ± 12 |
1097659 | ALS-31-7 | - | 2 | - | - | 95.4 | 125.0 | n.d. |
1098702 | ALS-31-8 | 2 | 2 | CH3 |
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69.2 | 76.9 | 292 ± 30 |
1099294 | ALS-31-9 | - | - | - | - | 65.3 | 50.3 | 64 ± 15 |
6235929 | ALS-31-10 | 2 | - | - |
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75.0 | 68.9 | 139 ± 8 |
1098529 | ALS-31-11 | 2 | - | - |
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83.7 | 125.1 | n.d. |
1098688 | ALS-31-12 | 2 | 1 | H | H | 75.6 | 125.3 | n.d. |
(a) Activity of SmSOD in the absence of compound equal to 100. (b) Not determined.