Table 3. Influence of conjugates of aminoadamantanes with carbazole derivatives C-1 and C-2 (Fig. 1) on tubulin polymerization.
Compounds | (dA355/dt)max, % (at 100 μM of compound) | |||
---|---|---|---|---|
No | R | R1 | R2 | 100 ± 14 |
C-1a | H | H | H | 192 ± 14 |
C-1b | H | H | CH3 | 249 ± 16 |
C-1c | Br | Br | H | 124 ± 17 |
C-1d | Br | Br | CH3 | 104 ± 24 |
C-1e | CI | CI | H | 100 ± 8 |
C-1f | CI | CI | CH3 | 101 ± 15 |
C-2a | H | H | H | 155 ± 22 |
C-2b | H | H | CH3 | 127 ± 10 |
C-2c | CH3 | H | H | 152 ± 12 |
C-2d | CH3 | H | CH3 | 182 ± 16 |
C-2e | CH3 | CH3 | H | 158 ± 19 |
C-2f | CH3 | CH3 | CH3 | 133 ± 14 |
C-2g | F | H | H | 164 ± 18 |
C-2h | F | H | CH3 | 330 ± 40 |
Memantine | 89 ± 7 | |||
Amantadine | 98 ± 16 | |||
Carbazole | 123 ± 12 | |||
Paclitaxel (5 μM) | 487 ± 32 |
Data presented as percent of maximum rate of 355 nm absorbance increase due to microtubules assembly. 100% - maximum rate of 355 nm absorbance in control probe with only vehicle (10% of DMSO).