Table 1. In Vitro Antimalarial Activity, Cytotoxicity, and SIs of 3-APA Analogs.
IC50 (μM) ± SDa |
|||
---|---|---|---|
compound | P. falciparum (W2) | Wi-26VA4 | SIb |
4a | 53.7 ± 0.7 | >300 | >5.6 |
4b | 37.7 ± 0.2 | 37.8 ± 5.0 | 1.0 |
4c | 14.0 ± 0.6 | 6.4 ± 0.7 | 0.4 |
4d | 8.9 ± 0.4 | 11.3 ± 1.4 | 1.2 |
5a | 210.6 ± 12.7 | >400 | 1.9 |
5b | >188 | 167.7 ± 10.5 | ND |
5c | 14.7 ± 0.2 | 99.1 ± 11.2 | 6.7 |
5d | 15.1 ± 0.8 | 34.1 ± 6.5 | 2.2 |
6a | 180.2 ± 8.3 | NDc | ND |
6b | 52.4 ± 8.9 | ND | ND |
6c | 20.3 ± 0.2 | ND | ND |
6d | 30.6 ± 2.7 | ND | ND |
CQd | 0.4 ± 0.066 | >100 | >250 |
SD: standard deviation.
SI: selectivity index.
ND: not determined.
CQ: chloroquine.