TABLE 5.
Comparison of in vitro data and yeast sensitivity to NCI compounds
| Compound | IC50 (μM) for enzyme in vitro
|
Yeast inhibition (cm in spoke assay)a
|
||||
|---|---|---|---|---|---|---|
| Cp-yeast type I | Cp-yeast type II | Hu-yeast | Cp-yeast type I | Cp-yeast type II | Hu-yeast | |
| Trimetrexate | 0.004 | 0.001 | 0.001 | 2.3 | 2.5 | 2.9 |
| 61670 | >1,000 | NDb | 700 | − | − | − |
| 104126 | >100 | >100 | >100 | − | − | − |
| 106568 | 5 | 2 | 500 | 1.5 | 2 | − |
| 107242 | >100 | >100 | 300 | − | − | − |
| 112421 | 0.07 | 0.1 | 0.2 | 1.2 | 1.6 | 1.4 |
| 117288 | >1,000 | ND | >1,000 | 0.6 | 0.6 | 0.7 |
| 121146 | 0.006 | 0.01 | 0.1 | 1.1 | 1.2 | 1.5 |
| 3081 | 200 | 60 | 5 | − | − | 1.8 |
| 47532 | >200 | >10 | >100 | − | − | − |
| 77028 | >100 | >100 | 50 | − | − | − |
| 104133 | 80 | 30 | 2 | − | − | 0.9 |
| 114923 | 30 | 20 | 2 | − | − | − |
| 127916 | >100 | >100 | 20 | − | − | − |
| Chlorasquin | 0.001 | 0.0007 | 0.0009 | 1.9 | 2.2 | 2.1 |
a
Duplicates data in Table 4. −, no inhibition detected.
b
ND, not done.