Table 1. In vitro potency and hypoxia cytotoxicity ratio (HCR) in A549 human cancer cell line.
| Compound | IC50 [oxic] (μM) ± SEMa,b | IC50 [anoxic] (μM) ± SEMa,b | HCR |
|---|---|---|---|
| TPZ (1) | 63.5 | 7.1 | 8.9 |
| OXi6196 (2) | 0.0066c | NDd | NDd |
| KGP18 (3) | 0.000027c | NDd | NDd |
| OXi8006 (4) | 0.030c | NDd | NDd |
| KGP24 (12) | 0.46 ± 0.05 | 0.48 ± 0.04 | 1.0 |
| KGP25 (13) | 2.74 ± 1.13 | 0.25 ± 0.08 | 11.0 |
| KGP66 (14) | 0.13 ± 0.06 | 0.05 ± 0.01 | 2.6 |
| KGP105 (15) | 0.25 ± 0.02 | 0.04 ± 0.003 | 6.2 |
| KGP291 (16) | 0.38 ± 0.03 | 0.05 ± 0.004 | 7.6 |
| KGP30 (17)e | NDd | NDd | NDd |
| KGP29 (18)e | NDd | NDd | NDd |
| KGP305 (19) | 0.05 ± 0.005 | 0.22 ± 0.09 | 0.2 |
| KGP304 (20) | 2.27 ± 1.01 | 0.38 ± 0.12 | 6.0 |
| KGP293 (21) | 0.36 ± 0.02 | 0.04 ± 0.005 | 9.0 |
| KGP292 (22) | 0.67 ± 0.13 | 0.14 ± 0.04 | 4.8 |
| KGP311 (23) | 5.58 ± 3.59 | 0.07 ± 0.04 | 79.7 |
| KGP343 (24) | 4.06 ± 1.89 | 0.12 ± 0.06 | 33.8 |
| KGP354 (25) | 5.53 ± 2.22 | 0.07 ± 0.02 | 79 |
Average of n ≥ 3 independent determinations.
4 h incubation (oxic or anoxic) followed by 48 h oxic exposure.
Values for standard SRB assay for cytotoxicity in A549 cells.
ND = not determined.
See Table S3 for HCR data under different assay conditions.