Table 1. Cytotoxic Activities of 2,4-Diaminopteridine Derivatives on HeLa Cancer Cells and Ect1/E6E7 Normal Cells with (4 Gy) or without (0 Gy) X-rays by MTT Assay.
| IC50 (μM) |
|||||||
|---|---|---|---|---|---|---|---|
| 2a | 2b | 2c | 2d | 2e | 2f | MTX | |
| HeLa + 0 Gy | 2.1 ± 0.2 | >80 | 9.8 ± 0.3 | 32.6 ± 1.2 | 24.5 ± 1.2 | 4.6 ± 0.3 | 1.5 ± 0.2 |
| HeLa + 4 Gy | 0.64 ± 0.03 | >80 | 6.3 ± 0.2 | 14.8 ± 0.4 | 14.6 ± 0.8 | 2.3 ± 0.2 | 0.82 ± 0.08 |
| SERa | 3.3 ± 0.2 | NA | 1.6 ± 0.1 | 2.20 ± 0.2 | 1.7 ± 0.1 | 2.0 ± 0.4 | 1.8 ± 0.3 |
| Ect1/E6E7 + 0 Gy | 6.9 ± 0.3 | >80 | 20.0 ± 1.0 | 59.3 ± 1.6 | 40.1 ± 1.6 | 10.9 ± 1.8 | 2.9 ± 0.3 |
| Ect1/E6E7 + 4 Gy | 3.1 ± 0.2 | >80 | 13.9 ± 1.0 | 38.1 ± 1.9 | 19.8 ± 1.2 | 5.3 ± 0.3 | 1.8 ± 0.2 |
| SERb | 2.2 ± 0.1 | NA | 1.4 ± 0.2 | 1.6 ± 0.1 | 2.0 ± 0.1 | 2.1 ± 0.2 | 1.6 ± 0.3 |
| SI0c | 3.3 ± 0.4 | NA | 2.0 ± 0.1 | 1.8 ± 0.1 | 1.6 ± 0.1 | 2.5 ± 0.3 | 1.9 ± 0.2 |
| SI4d | 4.8 ± 0.5 | NA | 2.2 ± 0.1 | 2.6 ± 0.1 | 1.4 ± 0.1 | 2.3 ± 0.4 | 2.2 ± 0.1 |
Sensitivity enhancement ratio (SER) = IC50(HeLa + 0 Gy)/IC50(HeLa + 4 Gy).
SER = IC50 (Ect1/E6E7 + 0 Gy)/IC50 (Ect1/E6E7 + 4 Gy).
Safe index for 0 Gy (SI0) = (Ect1/E6E7 + 0 Gy)/(HeLa + 0 Gy).
Safe index for 4 Gy (SI4) = (Ect1/E6E7 + 4 Gy)/(HeLa + 4 Gy).