Table 3.
Selectivity of polyamine analogues for growth inhibition of P. falciparum (3D7) compared to selected mammalian cells.
| Cpd | P. falciparum (IC50, μM) | Calu-6 (GI50, μM)a | HepG2 (GI50, μM) | SIc (Calu-6/Pf) | SIc (HepG2/Pf) |
|---|---|---|---|---|---|
| 9 | 0.144 ± 0.031 | 23.92 ± 0.4 | 166 | ||
| 13 | 0.253 ± 0.003 | 24.52 ± 1.4 | 97 | ||
| 14 | 1.316 ± 0.01 | 9.4 | nd | 7 | - |
| 15 | 0.329 ± 0.009 | 38.3 | 18.92 ± 1.39 | 38 | 58 |
| 16 | 0.405± 0.008 | 10.3 | 24.67 ± 0.3 | 25 | 61 |
| 20 | 0.355 ± 0.09 | >200 | >500 | ||
| 25 | 0.211 ± 0.007 | >200 | >500 | ||
| 29 | 0.106 ± 0.011 | >200 | >1500 | ||
| 30 | 0.088 ± 0.007 | 619.3 ± 25.8d | 7038 | ||
| 38 | 0.130 ± 0.002 | >200 | >1500 | ||
| 39 | 0.1 ± 0.003 | 33.8 ± 3.24 | 338 | ||
| CQ | 0.009 | 22.16 ± 0.39 | 2462 |
a
Data obtained from Sharma et al.13 Calu-6 are human nonsmall cell lung carcinoma cells
b
Values are the means ± S.E. of at least 2 independent experiments performed in duplicate. HepG2 are human hepatocellular liver carcinoma cells.
c
Selectivity indices were determined as the compound GI50 mammalian cell/IC50 P. falciparum
d
Values are the means ± S.E. of 3 independent experiments performed in duplicate.