Table 6. Abbott quinobenoxazine series SAR. Significantly, a much lower susceptibility to MDR efflux was displayed by quinolones in this series compared to doxorubicin (wild type P388 vs P388 (ADR) lines).
| Compound | R5 | R7 | a/b |
Min. DNA un-winding conc.a
(μg/mL) |
Decatenation inhib.b
(μg/mL) |
A549c
CC50 (μg/mL) |
P388d
CC50 (μg/mL) |
P388/
ADRe (MDR) CC50 (μg/mL) |
|---|---|---|---|---|---|---|---|---|
|
doxof 13 |
- | - | - | * | * | 0.31 | 0.0015 | 2.59 |
| 55g | H | A | H/H | 0.5 | 0.45 | 0.26 | 0.019 | 0.12 |
| 55(R)h | H | A | H/H | * | * | 0.42 | 0.021 | 0.10 |
| 55(S)i | H | A | H/H | * | * | 0.23 | 0.017 | 0.12 |