Table 5.
Folate receptor-dependent anti-proliferative activity of folate- and pteroate-derived hydroxamates (IC50 in μM).
| |||||
|---|---|---|---|---|---|
| R | n | KB | HeLa | A549 | |
|
11a | 1 | NI | NI | NT |
| 11b | 2 | NI | NI | NT | |
| 11c | 3 | 25 ± 2%† | NI | NT | |
| 11d | 4 | 53.7 ± 2.4 | 34 ± 3%† | NI | |
| 11e | 5 | 30.3 ± 2.1 | 56.6 ± 1.1 | NI | |
| 11f | 6 | 33 ± 3%† | 35 ± 3%† | NT | |
| 11g | 7 | 47 ± 3%† | 36 ± 8%† | NT | |
|
| |||||
|
15a | 1 | NT | NT | NT |
| 15b | 4 | NI | NI | NT | |
| 15c | 5 | NI | NI | NT | |
| 15d | 6 | NT | NT | NT | |
|
| |||||
| SAHA | - | 1.8 ± 0.3 | 3.7 ± 0.2 | NT | |
NI: No inhibition (below 20% inhibition at 100 μM);
: % inhibition at 100μM;
NT: Not tested.