Table 1.
R1 | Compound | n | IC50 |
---|---|---|---|
Unsubstituted pyridinium salts (R2 = H) | |||
1 | 4 | >30 | |
2 | 6 | >30 | |
3, MRS 2481 | 8 | 1.81 ± 0.58 | |
4 | 10 | 2.52 ± 0.39 | |
5, MRS 2485 | 8 | >25 | |
6 | 8 | >30 | |
7 | 8 | 12 ± 0.8 | |
8 | 8 | 3.16 ± 0.52 | |
9 | 8 | >30 | |
10 | 8 | >30 | |
11 | 8 | >30 | |
12 | 8 | >30 | |
13 | 8 | >30 | |
14 | 8 | Toxic at 1 μM | |
15 | 8 | 2.2 ± 0.8 | |
16 | 8 | 4.6 ± 0.9 | |
17 | 8 | >30 | |
R1 | Compound | R2 | IC50 |
Substituted pyridinium salts and other derivatives, n = 8 | |||
18 | 3-CONH2 | 5.56 ± 0.98 | |
19 | p-(CH2)2CH3 | 3.3 ± 0.5 | |
20 | p-(CH2)2-OH | 18 ± 0.9 | |
21 | 24 ± 1.0 | ||
22 | >30 |
The IC50 determinations were performed in duplicate at concentrations ranging from 0.3 to 10 μM on IB-3 cells grown in 96-well microtiter plates (n = 3, or more). The solvent control containing EtOH or DMSO for initial dissolution of the compounds, which at the concentration selected minimally deviates from medium alone, is then used as a basis for 100% activity.