The differential efficacy of NAT ligands and their Fe(iii), Cu(ii), and Zn(ii) complexes relative to Dp44mT and DpC to inhibit proliferation (IC50; μM) of KBV1 (+Pgp) and KB31 (−Pgp) cells after incubations of 24, 48, or 72 h/37 °C. The results are mean ± SD (3 experiments).
Compounds | IC50 values (μM) | ||||||||
---|---|---|---|---|---|---|---|---|---|
24 h | Fold dif. | 48 h | Fold dif. | 72 h | Fold dif. | ||||
KBV1 | KB31 | KBV1 | KB31 | KBV1 | KB31 | ||||
Dp44mT | 2.39 ± 0.12 | 8.16 ± 0.88 | 3.42 | 0.23 ± 0.01 | 2.45 ± 0.24 | 10.54 | 0.01 ± 0.002 | 0.13 ± 0.02 | 10.68 |
DpC | 1.31 ± 0.09 | 10.23 ± 0.7 | 7.82 | 0.16 ± 0.01 | 1.0 ± 0.05 | 6.71 | 0.19 ± 0.02 | 0.29 ± 0.07 | 1.53 |
AOBP | 2.12 ± 0.30 | 11.16 ± 1.04 | 5.12 | 0.74 ± 0.02 | 4.56 ± 0.32 | 6.19 | 0.61 ± 0.06 | 0.97 ± 0.22 | 1.60 |
[Fe(AOBP)2]+ | 10.93 ± 0.98 | 14.75 ± 1.98 | 1.35 | 0.40 ± 0.02 | 3.78 ± 0.75 | 9.42 | 0.25 ± 0.02 | 1.94 ± 0.24 | 7.68 |
[Cu(AOBP)2] | 2.13 ± 0.37 | 8.39 ± 0.98 | 3.95 | 0.26 ± 0.03 | 10.39 ± 0.52 | 39.72 | 0.14 ± 0.02 | 1.63 ± 0.34 | 11.66 |
[Zn(AOBP)2] | 3.25 ± 0.42 | >25 | >7.7 | 0.59 ± 0.01 | 4.74 ± 0.54 | 7.96 | 0.37 ± 0.08 | 2.78 ± 0.16 | 7.43 |
AODP | 5.75 ± 0.42 | 6.49 ± 0.86 | 1.13 | 0.55 ± 0.01 | 2.27 ± 0.31 | 4.09 | 0.46 ± 0.04 | 2.13 ± 0.22 | 4.61 |
[Fe(AODP)2]+ | 15.78 ± 1.97 | 17.66 ± 0.96 | 1.12 | 0.22 ± 0.03 | 5.23 ± 0.41 | 23.59 | 0.30 ± 0.010 | 2.40 ± 0.41 | 7.95 |
AOAPZ | 5.43 ± 0.33 | 5.14 ± 0.86 | 0.95 | 1.32 ± 0.06 | 4.43 ± 0.39 | 3.36 | 1.42 ± 0.26 | 3.55 ± 0.51 | 2.49 |
[Cu(AOAPZ)2] | 3.89 ± 0.18 | 3.73 ± 0.32 | 0.96 | 2.49 ± 0.05 | 3.64 ± 0.13 | 1.46 | 1.50 ± 0.19 | 2.84 ± 0.71 | 1.89 |
[Zn(AOAPZ)2] | 12.13 ± 1.84 | 18.17 ± 2.46 | 1.49 | 0.63 ± 0.04 | 4.33 ± 0.45 | 6.85 | 0.69 ± 0.12 | 1.72 ± 0.18 | 2.47 |
AOAP | 6.56 ± 0.74 | 7.95 ± 0.99 | 1.21 | 2.29 ± 0.18 | 4.62 ± 0.31 | 2.01 | 1.69 ± 0.33 | 2.12 ± 0.38 | 1.25 |
[Fe(AOAP)2]+ | >25 | >25 | — | 1.21 ± 0.22 | 19.58 ± 2.03 | 7.96 | 2.09 ± 0.39 | >5 | >2.38 |
[Cu(AOAP)2] | 2.96 ± 0.38 | 4.21 ± 0.68 | 1.42 | 2.46 ± 0.06 | 3.23 ± 0.26 | 1.31 | 0.87 ± 0.161 | 2.56 ± 0.61 | 2.97 |