Table 2.
In vitro activity against antiplasmodial and cytotoxic activity.
| Compoundc | Structure | P. falca EC50(μM) |
L-6 cellsb EC50(μM) |
cLogP | CLogD pH 7.4 |
|---|---|---|---|---|---|
| 33 |  |
2.6 | >230 | 4.5 | 1.8 |
| 34 |  |
2.2 | >200 | 5.7 | 2.6 |
| 35 |  |
1.5 | 120 | 4.5 | 2.4 |
| 36 |  |
0.99 | >210 | 3.3 | 1.1 |
| 37 |  |
3.9 | >240 | 4.0 | 1.3 |
| 38 |  |
4.6 | 180 | 4.3 | 1.9 |
| 39 |  |
>13 | >220 | 3.2 | 1.2 |
| 40 |  |
5.6 | 78 | 2.0 | −0.14 |
| 41 |  |
4.7 | 4 | 3.7 | 1.1 |
| 42 |  |
9.5 | >290 | 2.8 | 0.10 |
| 43 |  |
3.6 | 34 | 3.1 | 0.7 |
| 44 |  |
1.9 | 64 | 4.0 | 4.0 |
| 45 |  |
2.2 | >290 | 3.4 | 3.4 |
| 46 |  |
8.4 | 43 | 4.0 | 4.0 |
| 47 |  |
5.8 | 56 | 4.0 | 1.8 |
| 48 |  |
21 | 9 | 4.2 | 4.2 |
| 49 |  |
13 | 84 | 3.4 | 3.4 |
| 50 |  |
11 | >320 | 2.3 | 2.3 |
| 51 |  |
16 | 120 | 2.9 | 2.9 |
| 52 |  |
29 | 16 | 3.3 | 3.3 |
a
Plasmodium falciparum.
b
Measure of cytotoxicity; nd: not determined. Controls: for P. falciparum, chloroquine K1, EC50 = 0.1 μg/ml; for cytotoxicity (L6 cells), podophyllotoxin, EC50 = 0.005 μg/ml. The EC50 values are the data are means of two independent assays run in singleton. Yields for compounds 33–52, 40–80%.
c
Configuration as (Z,Z) 33–44, as (Z) 45,49–50, as (E) 46–48.