Table 3.
Biological data of novel analogues 5–8 in comparison to archazolid F (3) and archazolog 4.
|
|
3 |
4 |
5 |
6 |
7 |
8 |
|---|---|---|---|---|---|---|
|
Growth inhibition of 1321 N1 astrocytoma cells IC50±SEM [nM] |
4.51±0.51 |
0.757±0.121 |
12.2±2.9 |
19.6±4.0 |
9.65±1.48 |
17.4±1.30 |
|
Human P2X3 inhibition IC50± SEM [μM] |
0.438± 0.144 |
1.31±0.19 |
2.46±0.46 |
1.19±0.18 |
1.02±0.24 |
1.87±0.03 |
|
Affinity for the human adenosine A3 receptor K i±SEM [nM] |
859±75 |
690±39 |
539±44 |
436±111 |
>1000 |
>1000 |
|
HLE inhibition K i±SEM [μM] |
0.830±0.134 |
5.85±0.16 |
5.01±0.79 |
13.3±1.5 |
5.78±0.65 |
8.18±1.01 |