Table 1.
Selected RCQ Activities against P. falciparum [14]
| Compound | ClogP a | IC50 b(nM) | IC50 Ratio Dd2/D6 | Cytotoxicity c(nM) | ||
|---|---|---|---|---|---|---|
| D6 (CQS) | Dd2 (CQR) | |||||
| CQ |  |
5.1 | 7 | 102 | 15 | 12000 |
| 1 |  |
8.9 | 3 | 5 | 1.7 | 700 |
| 2 |  |
3.5 | 1.6 | 1.8 | 1.1 | 6500 |
| 3 |  |
7.5 | 1.3 | 1.3 | 1.0 | 1100 |
| 4 |  |
7.0 | 10 | 16 | 1.6 | 2200 |
| 5 |  |
7.3 | 7 | 16 | 2.3 | N.D. |
| 6 |  |
7.3 | 2 | 6 | 3.0 | N.D. |
| 7 |  |
7.6 | 23 | 34 | 1.5 | 700 |
| 8 |  |
7.4 | 8 | 11 | 1.4 | 1300 |
a
Evaluated using ChemDraw software.
b
Averages of at least 3 runs (± 15%). The uncertainties are estimated based on weighing uncertainties for the various compounds (which are free-bases and often oils), as well as on variability between determinations that were performed on different weeks.
c
Cytotoxicities are against mouse spleen lymphocytes. These values are estimated to be ±50%, based on weighing uncertainties for the various compounds (which are free-bases and often oils), as well as on variability between determinations that were performed on different weeks. N.D.: not determined.