Table 1.
Compound | IC50 (µM) ± SDa | IMAX (%) ± SDb | IG50 (µM) ± SDc | TRd |
---|---|---|---|---|
5a | 0.25 ± 0.01 | 72.55 ± 3.72 | > 100 | > 393.60 |
5b | 0.45 ± 0.10 | 112.80 ± 3.67 | 12.58 ± 5.12 | 28.10 |
5c | 0.65 ± 0.03 | 60.05 ± 4.04 | 36.50 ± 20.08 | 56.41 |
5d | 2.71 ± 0.14 | 68.50 ± 0.68 | 26.70 ± 5.52 | 9.85 |
5e | 0.15 ± 0.08 | 36.88 ± 1.16 | 66.50 ± 7.78 | 453.11 |
5f. | 0.18 ± 0.02 | 48.39 ± 0.80 | 27.35 ± 7.57 | 153.24 |
5g | 0.44 ± 0.03 | 65.23 ± 0.94 | 25.95 ± 14.35 | 58.79 |
5h | 0.42 ± 0.07 | 69.62 ± 1.14 | 24.25 ± 3.32 | 57.21 |
5i | 0.07 ± 0.02 | 62.83 ± 0.48 | 19.80 ± 3.39 | 293.66 |
5j | 0.48 ± 0.08 | 85.57 ± 2.59 | 15.65 ± 7.28 | 32.86 |
5k | 0.92 ± 0.10 | 115.70 ± 2.36 | 21.10 ± 2.55 | 22.85 |
5l | 0.24 ± 0.03 | 82.35 ± 3.44 | 14.25 ± 0.07 | 59.72 |
5m | 0.19 ± 0.07 | 87.42 ± 2.46 | 12.60 ± 7.22 | 66.23 |
5n | 4.09 ± 0.56 | 133.18 ± 3.35 | 21.50 ± 5.09 | 5.26 |
6a | 0.21 ± 0.03 | 62.65 ± 2.30 | > 100 | > 469.65 |
6c | 0.48 ± 0.10 | 90.51 ± 8.07 | 39.05 ± 26.94 | 81.35 |
6d | 0.19 ± 0.04 | 84.79 ± 2.51 | 33.30 ± 13.86 | 176.12 |
6e | 0.20 ± 0.04 | 66.80 ± 1.79 | 41.50 ± 33.52 | 212.38 |
p4he,19 | 0.23 ± 0.02 | 100.00 ± 21.00 | > 100 | > 435.00 |
p4je,19 | 0.21 ± 0.07 | 106.00 ± 21.00 | 27.20 ± 0.70 | 130.00 |
p4ke,19 | 0.31 ± 0.09 | 78.00 ± 14.00 | 12.70 ± 3.10 | 41.00 |
p5he,20 | 0.15 ± 0.01 | 85.00 ± 11.00 | 54.00 ± 14.00 | 360.00 |
aThe affinity of inhibitor interaction was expressed as IC50 values (compound concentrations giving a half-maximal inhibition).
bThe maximal inhibition percentage (IMAX) was determined by IC50 fitted curves.
cThe cytotoxicity was expressed as IG50 values (compound concentrations giving a half-maximal cell viability).
dThe therapeutic ratio (TR) corresponds to the ratio between IG50 and IC50 values.
eExperimental data of compounds p4h, p4j, p4k and p5h correspond to those previously published.