Table 1.
In vitro cytotoxic activity of compounds 1–13
| Compound | A549 (μM) | HT29 (μM) | MDA-MB-231 (μM) | PSN1 (μM) | |
|---|---|---|---|---|---|
|
1
PM100117 |
GI50 | 1.52 | 3.04 | 2.66 | nd |
| TGI | 1.84 | 3.23 | 2.79 | nd | |
| LC50 | 2.22 | 3.61 | 2.97 | nd | |
|
2
PM100118 |
GI50 | 2.24 | 1.92 | 1.73 | nd |
| TGI | 3.13 | 2.81 | 2.75 | nd | |
| LC50 | 4.28 | 4.09 | 4.16 | nd | |
|
3
From mutant ΔgonCM |
GI50 | 1.94 | 5.03 | 4.06 | 2.97 |
| TGI | 2.39 | 6.07 | 6.39 | 3.23 | |
| LC50 | 3.16 | >6.45 | >6.45 | >6.45 | |
|
4
From mutant ΔgonCM |
GI50 | 2.02 | 5.22 | 4.39 | 3.13 |
| TGI | 2.58 | 6.76 | 5.78 | 3.41 | |
| LC50 | >6.97 | >6.97 | >6.76 | >6.97 | |
|
5
From mutant ΔgonD3 |
GI50 | >6.82 | >6.82 | >6.82 | >6.82 |
| TGI | nd | nd | nd | nd | |
| LC50 | nd | nd | nd | nd | |
|
6, 7, 8 and 9
From mutant ΔgonE a |
GI50 | >10.70 | >10.70 | >10.70 | >10.70 |
| TGI | nd | nd | nd | nd | |
| LC50 | nd | nd | nd | nd | |
|
10
From mutant ΔgonG1 |
GI50 | >10.70 | >10.70 | >10.70 | >10.70 |
| TGI | nd | nd | nd | nd | |
| LC50 | nd | nd | nd | nd | |
|
11 and 12
From mutant ΔgonG2 a |
GI50 | >9.20 | >9.20 | >9.20 | >9.20 |
| TGI | nd | nd | nd | nd | |
| LC50 | nd | nd | nd | nd | |
|
13
From mutant ΔgonG3 |
GI50 | >6.90 | >6.90 | >6.90 | >6.90 |
| TGI | nd | nd | nd | nd | |
| LC50 | nd | nd | nd | nd | |
aThese compounds were assayed individually
GI 50 compound concentration that produces 50% inhibition on cell growth as compared to control cells, TGI compound concentration that produces total growth inhibition as compared to control cells, LC 50 compound concentration that produces 50% cell death as compared to control cells, nd values not determined