TABLE 4.
Susceptibility of L. major and differentiated THP-1 cells to nitrobenzyl phosphoramide mustards
| Compounds |
L. major IC50 |
Differentiated THP-1 IC50b | Selective toxicityc | |
|---|---|---|---|---|
| Promastigotesa | Amastigotesb | |||
| μm | μm | |||
| Nifurtimox | 6.28 ± 0.04 | 2.15 ± 0.01 | >100.00 | >47 |
| LH3–9, LH12–15, LH17–18, LH24 | >30.00 | >10.00 | NDd | ND |
| LH16 | 15.60 ± 1.13 | 2.75 ± 0.40 | >100.00 | >36 |
| LH19 | >30.00 | 4.72 ± 0.55 | >100.00 | >21 |
| LH27 | 16.23 ± 0.29 | 4.65 ± 0.15 | >100.00 | >22 |
| LH31 | 9.05 ± 0.56 | 7.00 ± 0.40 | >100.00 | >14 |
| LH32 | 4.72 ± 0.23 | 1.09 ± 0.21 | >100.00 | >92 |
| LH33 | 5.88 ± 0.28 | 0.21 ± 0.07 | >100.00 | >476 |
| LH34 | 3.10 ± 0.28 | 0.77 ± 0.12 | >100.00 | >143 |
| LH37 | 1.29 ± 0.08 | 2.17 ± 0.27 | >100.00 | >46 |
a Data are means from four experiments ± S.D.
b Data are means from three experiments ± S.D.
c The therapeutic index of a compound was calculated as a ratio of the IC50 value against differentiated THP-1 cells to the IC50 value against amastigote parasites.
d ND means not determined.