Table 1 Inhibitory activity against P. falciparum (reported and evaluated ICPf50, 3D7 strain), hepatocarcinoma cells using MTT assay
# | Code | Structure | Reported ICPf50 (µM) | ICPf50 (µM) Average (confidence interval-95%) | ICHepG2, MTT50 (µM) Average (confidence interval-95%) | ICHepG2, NR50 (µM) Average (confidence interval-95%) | SIMTT Average (confidence interval- 95%) | SINR Average (confidence interval-95%) |
|---|---|---|---|---|---|---|---|---|
01 | MMV006172 |
| 0.142 | 0.074 (0.072–0.076) | 3.21 (3.18–3.24) | 3.34 (3.28–3.40) | 43.4 (42.6–44.2) | 45.1 (44.6–45.6) |
02 | MMV665971 |
| 0.489 | 0.40 (0.39–0.41) | 22 (16–28) | 22 (18–26) | 60 (50–70) | 55 (46–64) |
03 | MMV007224 |
| 1.06 | 0.34 (0.29–0.39) | 5.1 (4.5–5.7) | > 6.25 | 15.1 (14.6–15.6) | > 16 |
04 | MMV666607 |
| 0.142 | 0.44 (0.36–0.52) | > 6.25 | > 6.25 | > 12 | > 12 |
05 | MMV020439 |
| 0.512 | 0.25 (0.16–0.34) | 90 (80–100) | > 100 | 340 (280–400) | > 290 |
06 | MMV665934 |
| 1.07 | 1.2 (0.5–1.9) | > 12.5 | > 12.5 | > 6.6 | > 6.6 |
07 | MMV007574 |
| 0.826 | 1.0 (0.8–1.2) | > 25 | > 25 | > 21 | > 21 |
08 | MMV085203 |
| 0.0053 | 0.0055 (0.005–0.006) | > 50 | 33 (28–38) | > 8300 | 6100 (5800–6400) |
09 | MMV085583 |
| 0.237 | 0.17 (0.14–0.20) | > 12.5 | > 12.5 | > 63 | > 63 |
10 | MMV018984 |
| 0.693 | 0.85 (0.78–0.92) | nd | nd | nd | nd |
11 | MMV019871 |
| 0.345 | 1.6 (1.5–1.7) | > 50 | > 50 | > 29 | > 29 |
Artesunate |
| 0.008 | 0.017 (0.016–0.018) | 110 (80–140) | 110 (80–140) | 7000 (6000–8000) | 7000 (6000–8000) | |
2 + artesunate | – | 0.015 (0.014–0.016) | 15.70 (15.64–15.74) | 13.0 (12.3–13.7) | 1030 (940–1120) | 850 (820–880) | ||
9 + artesunate | – | 0.013 (0.011–0.015) | > 12.5 | > 12.5 | > 840 | > 840 | ||
