Table 2.
Topo-IIα inhibition activity and antiproliferative activity (GI50/µM) of the fluorinated purine derivatives and QAP1.
| Compound | Topo-IIα inhibition/ 100 µM |
SK-BR-3 cells |
MCF-7 cells |
||
|---|---|---|---|---|---|
| GI50/µM | R2 | GI50/µM | R2 | ||
| 18 | + | 6.8 ± 0.8 | 0.975 | 14.5 ± 0.5 | 0.903 |
| 19b | + | 8.0 ± 0.8 | 0.936 | 46.3 ± 0.9 | 0.958 |
| 20 | + | 13.6 + 0.9 | 0.954 | 4.9 ± 0.3 | 0.966 |
| 21b | − | >100 | N/Aa | >100 | N/A |
| 22b | + | 2.0 + 0.9 | 0.988 | 13.6 ± 0.7 | 0.954 |
| 23b | + | 7.0 ± 0.9 | 0.981 | 3.2 ± 0.7 | 0.966 |
| 24b | − | >100 | N/A | >100 | N/A |
| 25b | + | 11.4 + 0.8 | 0.965 | >100 | N/A |
| QAP1 | + | 10.2 ± 0.9 | 0.977 | 32 ± 2 | 0.961 |
Not applicable.