In vitro cytotoxic activities and selectivity indices (SI) of piplartine–furoxan hybrids 7–9 as well as their precursors hydroxyfuroxans (4–6) and the natural product PPT (1) against different human cell lines using the CCK-8 assay.
| Compounds | IC50a (μM) | SIb | |||||
|---|---|---|---|---|---|---|---|
| MCF-7 | MCF10A | PC3 | PNT2 | OVCAR-3 | SIbreastc | SIprostated | |
| PPT (1) | 5.4 ± 0.4 | 5.3 ± 0.1 | 5.6 ± 0.6 | 8.5 ± 0.3 | 3.5 ± 0.2 | 1.0 | 1.5 |
| 4 | 2.1 ± 0.3 | 1.8 ± 0.7 | 7.2 ± 0.2 | 1.9 ± 0.6 | 3.3 ± 0.5 | 0.9 | 0.3 |
| 5 | 2.0 ± 0.5 | 1.7 ± 0.3 | 3.8 ± 0.6 | 12.9 ± 4.1 | 2.2 ± 0.1 | 0.9 | 3.4 |
| 6 | 4.3 ± 1.0 | 14.8 ± 1.9 | 0.13 ± 0.06 | 17.6 ± 4.0 | 0.04 ± 0.01 | 3.4 | 136.9 |
| 7 | 1.2 ± 0.4 | 3.5 ± 1.3 | 0.24 ± 0.01 | 17.8 ± 3.9 | 0.4 ± 0.1 | 3.0 | 75.5 |
| 8 | 1.1 ± 0.4 | 3.6 ± 0.2 | 0.13 ± 0.06 | 3.3 ± 0.3 | 0.3 ± 0.1 | 3.1 | 26.2 |
| 9 | 7.9 ± 0.4 | 123.3 ± 4.5 | 0.05 ± 0.04 | 14.1 ± 2.2 | 0.12 ± 0.10 | 15.7 | 285.1 |
| Cisplatine | 14.8 ± 4.5 | 5.1 ± 1.3 | 7.5 ± 0.5 | 6.6 ± 0.5 | 14.9 ± 2.1 | 0.3 | 0.9 |
a
Half maximum inhibitory concentration (IC50) values for each compound were calculated, and the data are expressed as the mean IC50 value (μM) ± SD from two independent experiments performed in triplicate per plate.
b
SI: selectivity index defined as the ratio between the IC50 value for the normal cell line and the IC50 value for the cancer cell line.
c
SIbreast = IC50 (MCF10A)/IC50 (MCF-7).
d
SIprostate = IC50 (PNT2)/IC50 (PC3).
e
Positive control.