Table 1.
Cytotoxicity of macrocyclic pyridyl polyoxazolesa
| IC50 (μM) |
||||
|---|---|---|---|---|
| Compound | RPMI 8402 | KB3-1 wt | KBV-1 + MDR1 | KBH5.0 + BCRP |
| HXDV | 0.6 | 0.4 | 8.5 | 0.5 |
| 6a | 1.05 | 1.2 | 4.5 | 1.5 |
| 6b | 0.3 | 0.15 | 2.0 | 1.0 |
| 7a | >5 | >5 | >5 | >5 |
| 8 | >10 | 4.0 | >10 | >10 |
| 11a | 1.0 | 0.26 | >10 | >10 |
| 11b | >10 | >10 | >10 | >10 |
| 13a | 0.3 | 0.06 | >10 | 1.0 |
| 13b | >10 | >10 | >10 | >10 |
| 15a | 0.12 | 0.12 | >10 | >10 |
| 15b | 1.0 | 0.6 | >10 | >10 |
| 17 | 0.17 | 0.07 b | >10 b | >10 b |
| 18 | 0.09 | 0.03 b | >10 b | 0.14 b |
| 19 | 0.18 | 0.04 b | >10 b | 0.55 b |
| 23a | 4.5 | 0.4 | >10 | >10 |
| 23b | 1.0 | 1.0 | >10 | >10 |
| 23c | >10 | >10 | >10 | >10 |
| 23d | 5.0 | 3.0 | >10 | >10 |
a
Values represent the average of three experiments.
b
Values represent the average of four experiments.